BindingDB logo
myBDB logout
Compile Data Set for Download or QSAR

Found 57 hits of ec50 for UniProtKB: P21761   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kcal/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50072394
PNG
(1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...)
Show SMILES NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1 |r|
Show InChI InChI=1S/C16H22N6O4/c17-14(24)12-2-1-5-22(12)16(26)11(6-9-7-18-8-19-9)21-15(25)10-3-4-13(23)20-10/h7-8,10-12H,1-6H2,(H2,17,24)(H,18,19)(H,20,23)(H,21,25)/t10-,11-,12-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
Purchase

KEGG
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 0.490n/an/an/an/a



Washington University

Curated by ChEMBL


Assay Description
Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol


Bioorg Med Chem Lett 8: 3093-6 (1999)


Article DOI: 10.1016/S0960-894X(98)00567-8
BindingDB Entry DOI: 10.7270/Q21R6PP1
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50072394
PNG
(1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...)
Show SMILES NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1 |r|
Show InChI InChI=1S/C16H22N6O4/c17-14(24)12-2-1-5-22(12)16(26)11(6-9-7-18-8-19-9)21-15(25)10-3-4-13(23)20-10/h7-8,10-12H,1-6H2,(H2,17,24)(H,18,19)(H,20,23)(H,21,25)/t10-,11-,12-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
Purchase

KEGG
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 0.680n/an/an/an/a



Washington University

Curated by ChEMBL


Assay Description
Effective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cells


J Med Chem 39: 1571-4 (1996)


Article DOI: 10.1021/jm960053k
BindingDB Entry DOI: 10.7270/Q2H70GGR
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50072394
PNG
(1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...)
Show SMILES NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1 |r|
Show InChI InChI=1S/C16H22N6O4/c17-14(24)12-2-1-5-22(12)16(26)11(6-9-7-18-8-19-9)21-15(25)10-3-4-13(23)20-10/h7-8,10-12H,1-6H2,(H2,17,24)(H,18,19)(H,20,23)(H,21,25)/t10-,11-,12-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
Purchase

KEGG
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 1n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay


Eur J Med Chem 111: 72-83 (2016)


Article DOI: 10.1016/j.ejmech.2016.01.038
BindingDB Entry DOI: 10.7270/Q28G8NKF
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50072394
PNG
(1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...)
Show SMILES NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1 |r|
Show InChI InChI=1S/C16H22N6O4/c17-14(24)12-2-1-5-22(12)16(26)11(6-9-7-18-8-19-9)21-15(25)10-3-4-13(23)20-10/h7-8,10-12H,1-6H2,(H2,17,24)(H,18,19)(H,20,23)(H,21,25)/t10-,11-,12-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
Purchase

KEGG
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 1n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method


Bioorg Med Chem 23: 5641-53 (2015)


Article DOI: 10.1016/j.bmc.2015.07.022
BindingDB Entry DOI: 10.7270/Q2JH3NZ9
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50072394
PNG
(1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...)
Show SMILES NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1 |r|
Show InChI InChI=1S/C16H22N6O4/c17-14(24)12-2-1-5-22(12)16(26)11(6-9-7-18-8-19-9)21-15(25)10-3-4-13(23)20-10/h7-8,10-12H,1-6H2,(H2,17,24)(H,18,19)(H,20,23)(H,21,25)/t10-,11-,12-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
Purchase

KEGG
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 3.20n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA


Eur J Med Chem 111: 72-83 (2016)


Article DOI: 10.1016/j.ejmech.2016.01.038
BindingDB Entry DOI: 10.7270/Q28G8NKF
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50158418
PNG
(CHEMBL3780746)
Show SMILES Cn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Br |r|
Show InChI InChI=1S/C17H23BrN6O4/c1-23-8-9(20-17(23)18)7-11(22-15(27)10-4-5-13(25)21-10)16(28)24-6-2-3-12(24)14(19)26/h8,10-12H,2-7H2,1H3,(H2,19,26)(H,21,25)(H,22,27)/t10-,11-,12-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 3.40n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay


Eur J Med Chem 111: 72-83 (2016)


Article DOI: 10.1016/j.ejmech.2016.01.038
BindingDB Entry DOI: 10.7270/Q28G8NKF
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50158395
PNG
(CHEMBL3782037)
Show SMILES CCn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1I |r|
Show InChI InChI=1S/C18H25IN6O4/c1-2-24-9-10(21-18(24)19)8-12(23-16(28)11-5-6-14(26)22-11)17(29)25-7-3-4-13(25)15(20)27/h9,11-13H,2-8H2,1H3,(H2,20,27)(H,22,26)(H,23,28)/t11-,12-,13-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 4.90n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay


Eur J Med Chem 111: 72-83 (2016)


Article DOI: 10.1016/j.ejmech.2016.01.038
BindingDB Entry DOI: 10.7270/Q28G8NKF
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50158394
PNG
(CHEMBL3780645)
Show SMILES Cn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1I |r|
Show InChI InChI=1S/C17H23IN6O4/c1-23-8-9(20-17(23)18)7-11(22-15(27)10-4-5-13(25)21-10)16(28)24-6-2-3-12(24)14(19)26/h8,10-12H,2-7H2,1H3,(H2,19,26)(H,21,25)(H,22,27)/t10-,11-,12-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 5.90n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay


Eur J Med Chem 111: 72-83 (2016)


Article DOI: 10.1016/j.ejmech.2016.01.038
BindingDB Entry DOI: 10.7270/Q28G8NKF
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50158409
PNG
(CHEMBL3779931)
Show SMILES CCn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Br |r|
Show InChI InChI=1S/C18H25BrN6O4/c1-2-24-9-10(21-18(24)19)8-12(23-16(28)11-5-6-14(26)22-11)17(29)25-7-3-4-13(25)15(20)27/h9,11-13H,2-8H2,1H3,(H2,20,27)(H,22,26)(H,23,28)/t11-,12-,13-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 12n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay


Eur J Med Chem 111: 72-83 (2016)


Article DOI: 10.1016/j.ejmech.2016.01.038
BindingDB Entry DOI: 10.7270/Q28G8NKF
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50158395
PNG
(CHEMBL3782037)
Show SMILES CCn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1I |r|
Show InChI InChI=1S/C18H25IN6O4/c1-2-24-9-10(21-18(24)19)8-12(23-16(28)11-5-6-14(26)22-11)17(29)25-7-3-4-13(25)15(20)27/h9,11-13H,2-8H2,1H3,(H2,20,27)(H,22,26)(H,23,28)/t11-,12-,13-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 13n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA


Eur J Med Chem 111: 72-83 (2016)


Article DOI: 10.1016/j.ejmech.2016.01.038
BindingDB Entry DOI: 10.7270/Q28G8NKF
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50158401
PNG
(CHEMBL3780549)
Show SMILES NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(I)n(Cc2ccccc2)c1I)NC(=O)[C@@H]1CCC(=O)N1 |r|
Show InChI InChI=1S/C23H26I2N6O4/c24-19-15(29-23(25)31(19)12-13-5-2-1-3-6-13)11-16(28-21(34)14-8-9-18(32)27-14)22(35)30-10-4-7-17(30)20(26)33/h1-3,5-6,14,16-17H,4,7-12H2,(H2,26,33)(H,27,32)(H,28,34)/t14-,16-,17-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 15n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA


Eur J Med Chem 111: 72-83 (2016)


Article DOI: 10.1016/j.ejmech.2016.01.038
BindingDB Entry DOI: 10.7270/Q28G8NKF
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50109028
PNG
(CHEMBL3600447)
Show SMILES CCCc1nc(C[C@H](NC(=O)c2cnc(C)cn2)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1 |r|
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 17n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method


Bioorg Med Chem 23: 5641-53 (2015)


Article DOI: 10.1016/j.bmc.2015.07.022
BindingDB Entry DOI: 10.7270/Q2JH3NZ9
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50158396
PNG
(CHEMBL3781773)
Show SMILES NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cn(Cc2ccccc2)c(I)n1)NC(=O)[C@@H]1CCC(=O)N1 |r|
Show InChI InChI=1S/C23H27IN6O4/c24-23-26-15(13-29(23)12-14-5-2-1-3-6-14)11-17(28-21(33)16-8-9-19(31)27-16)22(34)30-10-4-7-18(30)20(25)32/h1-3,5-6,13,16-18H,4,7-12H2,(H2,25,32)(H,27,31)(H,28,33)/t16-,17-,18-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem
Article
PubMed
n/an/an/an/a 27n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA


Eur J Med Chem 111: 72-83 (2016)


Article DOI: 10.1016/j.ejmech.2016.01.038
BindingDB Entry DOI: 10.7270/Q28G8NKF
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50158418
PNG
(CHEMBL3780746)
Show SMILES Cn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Br |r|
Show InChI InChI=1S/C17H23BrN6O4/c1-23-8-9(20-17(23)18)7-11(22-15(27)10-4-5-13(25)21-10)16(28)24-6-2-3-12(24)14(19)26/h8,10-12H,2-7H2,1H3,(H2,19,26)(H,21,25)(H,22,27)/t10-,11-,12-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 28n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA


Eur J Med Chem 111: 72-83 (2016)


Article DOI: 10.1016/j.ejmech.2016.01.038
BindingDB Entry DOI: 10.7270/Q28G8NKF
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50158394
PNG
(CHEMBL3780645)
Show SMILES Cn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1I |r|
Show InChI InChI=1S/C17H23IN6O4/c1-23-8-9(20-17(23)18)7-11(22-15(27)10-4-5-13(25)21-10)16(28)24-6-2-3-12(24)14(19)26/h8,10-12H,2-7H2,1H3,(H2,19,26)(H,21,25)(H,22,27)/t10-,11-,12-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 31n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA


Eur J Med Chem 111: 72-83 (2016)


Article DOI: 10.1016/j.ejmech.2016.01.038
BindingDB Entry DOI: 10.7270/Q28G8NKF
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50158404
PNG
(CHEMBL3780373)
Show SMILES CCCn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Br |r|
Show InChI InChI=1S/C19H27BrN6O4/c1-2-7-25-10-11(22-19(25)20)9-13(24-17(29)12-5-6-15(27)23-12)18(30)26-8-3-4-14(26)16(21)28/h10,12-14H,2-9H2,1H3,(H2,21,28)(H,23,27)(H,24,29)/t12-,13-,14-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 32n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay


Eur J Med Chem 111: 72-83 (2016)


Article DOI: 10.1016/j.ejmech.2016.01.038
BindingDB Entry DOI: 10.7270/Q28G8NKF
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50158401
PNG
(CHEMBL3780549)
Show SMILES NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(I)n(Cc2ccccc2)c1I)NC(=O)[C@@H]1CCC(=O)N1 |r|
Show InChI InChI=1S/C23H26I2N6O4/c24-19-15(29-23(25)31(19)12-13-5-2-1-3-6-13)11-16(28-21(34)14-8-9-18(32)27-14)22(35)30-10-4-7-17(30)20(26)33/h1-3,5-6,14,16-17H,4,7-12H2,(H2,26,33)(H,27,32)(H,28,34)/t14-,16-,17-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 53n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay


Eur J Med Chem 111: 72-83 (2016)


Article DOI: 10.1016/j.ejmech.2016.01.038
BindingDB Entry DOI: 10.7270/Q28G8NKF
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50109039
PNG
(CHEMBL3600454)
Show SMILES Cc1cnc(cn1)C(=O)N[C@@H](Cc1nc(Br)[nH]c1Br)C(=O)N1CCC[C@H]1C(N)=O |r|
Show InChI InChI=1S/C17H19Br2N7O3/c1-8-6-22-11(7-21-8)15(28)23-10(5-9-13(18)25-17(19)24-9)16(29)26-4-2-3-12(26)14(20)27/h6-7,10,12H,2-5H2,1H3,(H2,20,27)(H,23,28)(H,24,25)/t10-,12-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 77n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method


Bioorg Med Chem 23: 5641-53 (2015)


Article DOI: 10.1016/j.bmc.2015.07.022
BindingDB Entry DOI: 10.7270/Q2JH3NZ9
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50050532
PNG
(1-[2-[2-oxo-(5S)-dihydro-2H-5-pyrrolylcarboxamido]...)
Show SMILES NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCC(=O)N1
Show InChI InChI=1S/C19H24N4O4/c20-17(25)15-7-4-10-23(15)19(27)14(11-12-5-2-1-3-6-12)22-18(26)13-8-9-16(24)21-13/h1-3,5-6,13-15H,4,7-11H2,(H2,20,25)(H,21,24)(H,22,26)/t13-,14-,15-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
Purchase

CHEMBL
MCE
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 110n/an/an/an/a



Washington University

Curated by ChEMBL


Assay Description
Effective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cells


J Med Chem 39: 1571-4 (1996)


Article DOI: 10.1021/jm960053k
BindingDB Entry DOI: 10.7270/Q2H70GGR
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50109027
PNG
(CHEMBL3600446)
Show SMILES CCCc1nc(C[C@H](NC(=O)c2cnccn2)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1 |r|
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 150n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method


Bioorg Med Chem 23: 5641-53 (2015)


Article DOI: 10.1016/j.bmc.2015.07.022
BindingDB Entry DOI: 10.7270/Q2JH3NZ9
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50158399
PNG
(CHEMBL3780802)
Show SMILES CCn1c(I)nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1I |r|
Show InChI InChI=1S/C18H24I2N6O4/c1-2-25-14(19)10(24-18(25)20)8-11(23-16(29)9-5-6-13(27)22-9)17(30)26-7-3-4-12(26)15(21)28/h9,11-12H,2-8H2,1H3,(H2,21,28)(H,22,27)(H,23,29)/t9-,11-,12-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 170n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA


Eur J Med Chem 111: 72-83 (2016)


Article DOI: 10.1016/j.ejmech.2016.01.038
BindingDB Entry DOI: 10.7270/Q28G8NKF
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50158399
PNG
(CHEMBL3780802)
Show SMILES CCn1c(I)nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1I |r|
Show InChI InChI=1S/C18H24I2N6O4/c1-2-25-14(19)10(24-18(25)20)8-11(23-16(29)9-5-6-13(27)22-9)17(30)26-7-3-4-12(26)15(21)28/h9,11-12H,2-8H2,1H3,(H2,21,28)(H,22,27)(H,23,29)/t9-,11-,12-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 249n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay


Eur J Med Chem 111: 72-83 (2016)


Article DOI: 10.1016/j.ejmech.2016.01.038
BindingDB Entry DOI: 10.7270/Q28G8NKF
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50158398
PNG
(CHEMBL3780633)
Show SMILES Cn1c(I)nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1I |r|
Show InChI InChI=1S/C17H22I2N6O4/c1-24-13(18)9(23-17(24)19)7-10(22-15(28)8-4-5-12(26)21-8)16(29)25-6-2-3-11(25)14(20)27/h8,10-11H,2-7H2,1H3,(H2,20,27)(H,21,26)(H,22,28)/t8-,10-,11-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 272n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay


Eur J Med Chem 111: 72-83 (2016)


Article DOI: 10.1016/j.ejmech.2016.01.038
BindingDB Entry DOI: 10.7270/Q28G8NKF
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50109040
PNG
(CHEMBL3601782)
Show SMILES NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc[nH]c1Br)NC(=O)c1nccnc1N |r|
Show InChI InChI=1S/C16H19BrN8O3/c17-12-8(22-7-23-12)6-9(16(28)25-5-1-2-10(25)14(19)26)24-15(27)11-13(18)21-4-3-20-11/h3-4,7,9-10H,1-2,5-6H2,(H2,18,21)(H2,19,26)(H,22,23)(H,24,27)/t9-,10-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 287n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method


Bioorg Med Chem 23: 5641-53 (2015)


Article DOI: 10.1016/j.bmc.2015.07.022
BindingDB Entry DOI: 10.7270/Q2JH3NZ9
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50050529
PNG
((S)-1-[2-((5R,7R)-2,6-Dioxo-1,7-diaza-spiro[4.4]no...)
Show SMILES NC(=O)[C@@H]1CCCN1C(=O)C(Cc1ccccc1)N1CC[C@]2(CCC(=O)N2)C1=O
Show InChI InChI=1S/C21H26N4O4/c22-18(27)15-7-4-11-24(15)19(28)16(13-14-5-2-1-3-6-14)25-12-10-21(20(25)29)9-8-17(26)23-21/h1-3,5-6,15-16H,4,7-13H2,(H2,22,27)(H,23,26)/t15-,16?,21+/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 290n/an/an/an/a



Washington University

Curated by ChEMBL


Assay Description
Effective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cells


J Med Chem 39: 1571-4 (1996)


Article DOI: 10.1021/jm960053k
BindingDB Entry DOI: 10.7270/Q2H70GGR
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50158532
PNG
(CHEMBL3781522)
Show SMILES Cn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Cl |r|
Show InChI InChI=1S/C17H23ClN6O4/c1-23-8-9(20-17(23)18)7-11(22-15(27)10-4-5-13(25)21-10)16(28)24-6-2-3-12(24)14(19)26/h8,10-12H,2-7H2,1H3,(H2,19,26)(H,21,25)(H,22,27)/t10-,11-,12-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Patents


Similars

Article
PubMed
n/an/an/an/a 320n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA


Eur J Med Chem 111: 72-83 (2016)


Article DOI: 10.1016/j.ejmech.2016.01.038
BindingDB Entry DOI: 10.7270/Q28G8NKF
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50158396
PNG
(CHEMBL3781773)
Show SMILES NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cn(Cc2ccccc2)c(I)n1)NC(=O)[C@@H]1CCC(=O)N1 |r|
Show InChI InChI=1S/C23H27IN6O4/c24-23-26-15(13-29(23)12-14-5-2-1-3-6-14)11-17(28-21(33)16-8-9-19(31)27-16)22(34)30-10-4-7-18(30)20(25)32/h1-3,5-6,13,16-18H,4,7-12H2,(H2,25,32)(H,27,31)(H,28,33)/t16-,17-,18-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem
Article
PubMed
n/an/an/an/a 339n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay


Eur J Med Chem 111: 72-83 (2016)


Article DOI: 10.1016/j.ejmech.2016.01.038
BindingDB Entry DOI: 10.7270/Q28G8NKF
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50109022
PNG
(CHEMBL3601785)
Show SMILES Cn1cnc(C[C@H](NC(=O)c2cnccn2)C(=O)N2CCC[C@H]2C(N)=O)c1Br |r|
Show InChI InChI=1S/C17H20BrN7O3/c1-24-9-22-10(14(24)18)7-11(23-16(27)12-8-20-4-5-21-12)17(28)25-6-2-3-13(25)15(19)26/h4-5,8-9,11,13H,2-3,6-7H2,1H3,(H2,19,26)(H,23,27)/t11-,13-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 340n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method


Bioorg Med Chem 23: 5641-53 (2015)


Article DOI: 10.1016/j.bmc.2015.07.022
BindingDB Entry DOI: 10.7270/Q2JH3NZ9
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50072395
PNG
(1-[3-cyclohexyl-2-(5-oxotetrahydro-1H-2-pyrrolylca...)
Show SMILES [H][C@]1(CCC(=O)N1)C(=O)N[C@@H](CC1CCCCC1)C(=O)N1CCC[C@H]1C(N)=O
Show InChI InChI=1S/C19H30N4O4/c20-17(25)15-7-4-10-23(15)19(27)14(11-12-5-2-1-3-6-12)22-18(26)13-8-9-16(24)21-13/h12-15H,1-11H2,(H2,20,25)(H,21,24)(H,22,26)/t13-,14-,15-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 430n/an/an/an/a



Washington University

Curated by ChEMBL


Assay Description
Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol


Bioorg Med Chem Lett 8: 3093-6 (1999)


Article DOI: 10.1016/S0960-894X(98)00567-8
BindingDB Entry DOI: 10.7270/Q21R6PP1
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50109041
PNG
(CHEMBL3601781)
Show SMILES Cc1cnc(cn1)C(=O)N[C@@H](Cc1nc[nH]c1Br)C(=O)N1CCC[C@H]1C(N)=O |r|
Show InChI InChI=1S/C17H20BrN7O3/c1-9-6-21-12(7-20-9)16(27)24-11(5-10-14(18)23-8-22-10)17(28)25-4-2-3-13(25)15(19)26/h6-8,11,13H,2-5H2,1H3,(H2,19,26)(H,22,23)(H,24,27)/t11-,13-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 498n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method


Bioorg Med Chem 23: 5641-53 (2015)


Article DOI: 10.1016/j.bmc.2015.07.022
BindingDB Entry DOI: 10.7270/Q2JH3NZ9
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50109025
PNG
(CHEMBL3600444)
Show SMILES Cc1cnc(cn1)C(=O)N[C@@H](Cc1nc(I)n(Cc2ccccc2)c1I)C(=O)N1CCC[C@H]1C(N)=O |r|
Show InChI InChI=1S/C24H25I2N7O3/c1-14-11-29-18(12-28-14)22(35)30-17(23(36)32-9-5-8-19(32)21(27)34)10-16-20(25)33(24(26)31-16)13-15-6-3-2-4-7-15/h2-4,6-7,11-12,17,19H,5,8-10,13H2,1H3,(H2,27,34)(H,30,35)/t17-,19-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 740n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method


Bioorg Med Chem 23: 5641-53 (2015)


Article DOI: 10.1016/j.bmc.2015.07.022
BindingDB Entry DOI: 10.7270/Q2JH3NZ9
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50158400
PNG
(CHEMBL3780191)
Show SMILES CCCn1c(I)nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1I |r|
Show InChI InChI=1S/C19H26I2N6O4/c1-2-7-27-15(20)11(25-19(27)21)9-12(24-17(30)10-5-6-14(28)23-10)18(31)26-8-3-4-13(26)16(22)29/h10,12-13H,2-9H2,1H3,(H2,22,29)(H,23,28)(H,24,30)/t10-,12-,13-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 780n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA


Eur J Med Chem 111: 72-83 (2016)


Article DOI: 10.1016/j.ejmech.2016.01.038
BindingDB Entry DOI: 10.7270/Q28G8NKF
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50158532
PNG
(CHEMBL3781522)
Show SMILES Cn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Cl |r|
Show InChI InChI=1S/C17H23ClN6O4/c1-23-8-9(20-17(23)18)7-11(22-15(27)10-4-5-13(25)21-10)16(28)24-6-2-3-12(24)14(19)26/h8,10-12H,2-7H2,1H3,(H2,19,26)(H,21,25)(H,22,27)/t10-,11-,12-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Patents


Similars

Article
PubMed
n/an/an/an/a 790n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay


Eur J Med Chem 111: 72-83 (2016)


Article DOI: 10.1016/j.ejmech.2016.01.038
BindingDB Entry DOI: 10.7270/Q28G8NKF
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50109034
PNG
(CHEMBL3600449)
Show SMILES CCCc1nc(C[C@H](NC(=O)[C@H]2CCCCN2)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1 |r|
Show InChI InChI=1S/C20H32N6O3/c1-2-6-17-23-12-13(24-17)11-15(25-19(28)14-7-3-4-9-22-14)20(29)26-10-5-8-16(26)18(21)27/h12,14-16,22H,2-11H2,1H3,(H2,21,27)(H,23,24)(H,25,28)/t14-,15+,16+/m1/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 940n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method


Bioorg Med Chem 23: 5641-53 (2015)


Article DOI: 10.1016/j.bmc.2015.07.022
BindingDB Entry DOI: 10.7270/Q2JH3NZ9
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50109026
PNG
(CHEMBL3600445)
Show SMILES NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(I)n(Cc2ccccc2)c1I)NC(=O)c1cnccn1 |r|
Show InChI InChI=1S/C23H23I2N7O3/c24-19-15(30-23(25)32(19)13-14-5-2-1-3-6-14)11-16(29-21(34)17-12-27-8-9-28-17)22(35)31-10-4-7-18(31)20(26)33/h1-3,5-6,8-9,12,16,18H,4,7,10-11,13H2,(H2,26,33)(H,29,34)/t16-,18-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 980n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method


Bioorg Med Chem 23: 5641-53 (2015)


Article DOI: 10.1016/j.bmc.2015.07.022
BindingDB Entry DOI: 10.7270/Q2JH3NZ9
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50109035
PNG
(CHEMBL3600450)
Show SMILES CC(C)c1nc(C[C@H](NC(=O)[C@H]2CCCCN2)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1 |r|
Show InChI InChI=1S/C20H32N6O3/c1-12(2)18-23-11-13(24-18)10-15(25-19(28)14-6-3-4-8-22-14)20(29)26-9-5-7-16(26)17(21)27/h11-12,14-16,22H,3-10H2,1-2H3,(H2,21,27)(H,23,24)(H,25,28)/t14-,15+,16+/m1/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 1.00E+3n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method


Bioorg Med Chem 23: 5641-53 (2015)


Article DOI: 10.1016/j.bmc.2015.07.022
BindingDB Entry DOI: 10.7270/Q2JH3NZ9
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50109017
PNG
(CHEMBL3601783)
Show SMILES NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(Br)[nH]c1Br)NC(=O)c1nccnc1N |r|
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Patents


Similars

Article
PubMed
n/an/an/an/a 1.41E+3n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method


Bioorg Med Chem 23: 5641-53 (2015)


Article DOI: 10.1016/j.bmc.2015.07.022
BindingDB Entry DOI: 10.7270/Q2JH3NZ9
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50109033
PNG
(CHEMBL3600448)
Show SMILES CCCc1nc(C[C@H](NC(=O)c2nccnc2N)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1 |r|
Show InChI InChI=1S/C19H26N8O3/c1-2-4-14-24-10-11(25-14)9-12(19(30)27-8-3-5-13(27)17(21)28)26-18(29)15-16(20)23-7-6-22-15/h6-7,10,12-13H,2-5,8-9H2,1H3,(H2,20,23)(H2,21,28)(H,24,25)(H,26,29)/t12-,13-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 1.56E+3n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method


Bioorg Med Chem 23: 5641-53 (2015)


Article DOI: 10.1016/j.bmc.2015.07.022
BindingDB Entry DOI: 10.7270/Q2JH3NZ9
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50072396
PNG
(7-cyclohexyl-6-(2,6-dioxo-1,7-diazaspiro[4.4]non-7...)
Show SMILES NC(=O)[C@@H]1CC[C@H]2CC(C3CCCCC3)=C(N3CC[C@]4(CCC(=O)N4)C3=O)C(=O)N12 |t:15|
Show InChI InChI=1S/C22H30N4O4/c23-19(28)16-7-6-14-12-15(13-4-2-1-3-5-13)18(20(29)26(14)16)25-11-10-22(21(25)30)9-8-17(27)24-22/h13-14,16H,1-12H2,(H2,23,28)(H,24,27)/t14-,16-,22+/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 1.80E+3n/an/an/an/a



Washington University

Curated by ChEMBL


Assay Description
Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol


Bioorg Med Chem Lett 8: 3093-6 (1999)


Article DOI: 10.1016/S0960-894X(98)00567-8
BindingDB Entry DOI: 10.7270/Q21R6PP1
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50158409
PNG
(CHEMBL3779931)
Show SMILES CCn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Br |r|
Show InChI InChI=1S/C18H25BrN6O4/c1-2-24-9-10(21-18(24)19)8-12(23-16(28)11-5-6-14(26)22-11)17(29)25-7-3-4-13(25)15(20)27/h9,11-13H,2-8H2,1H3,(H2,20,27)(H,22,26)(H,23,28)/t11-,12-,13-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 1.83E+3n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA


Eur J Med Chem 111: 72-83 (2016)


Article DOI: 10.1016/j.ejmech.2016.01.038
BindingDB Entry DOI: 10.7270/Q28G8NKF
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50158400
PNG
(CHEMBL3780191)
Show SMILES CCCn1c(I)nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1I |r|
Show InChI InChI=1S/C19H26I2N6O4/c1-2-7-27-15(20)11(25-19(27)21)9-12(24-17(30)10-5-6-14(28)23-10)18(31)26-8-3-4-13(26)16(22)29/h10,12-13H,2-9H2,1H3,(H2,22,29)(H,23,28)(H,24,30)/t10-,12-,13-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 2.40E+3n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay


Eur J Med Chem 111: 72-83 (2016)


Article DOI: 10.1016/j.ejmech.2016.01.038
BindingDB Entry DOI: 10.7270/Q28G8NKF
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50109038
PNG
(CHEMBL3600453)
Show SMILES NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(Br)[nH]c1Br)NC(=O)c1cnccn1 |r|
Show InChI InChI=1S/C16H17Br2N7O3/c17-12-8(23-16(18)24-12)6-9(22-14(27)10-7-20-3-4-21-10)15(28)25-5-1-2-11(25)13(19)26/h3-4,7,9,11H,1-2,5-6H2,(H2,19,26)(H,22,27)(H,23,24)/t9-,11-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 2.54E+3n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method


Bioorg Med Chem 23: 5641-53 (2015)


Article DOI: 10.1016/j.bmc.2015.07.022
BindingDB Entry DOI: 10.7270/Q2JH3NZ9
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50109037
PNG
(CHEMBL3600452)
Show SMILES NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc[nH]c1Br)NC(=O)c1cnccn1 |r|
Show InChI InChI=1S/C16H18BrN7O3/c17-13-9(21-8-22-13)6-10(23-15(26)11-7-19-3-4-20-11)16(27)24-5-1-2-12(24)14(18)25/h3-4,7-8,10,12H,1-2,5-6H2,(H2,18,25)(H,21,22)(H,23,26)/t10-,12-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 3.98E+3n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method


Bioorg Med Chem 23: 5641-53 (2015)


Article DOI: 10.1016/j.bmc.2015.07.022
BindingDB Entry DOI: 10.7270/Q2JH3NZ9
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50158397
PNG
(CHEMBL3780836)
Show SMILES NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(Cl)[nH]c1Cl)NC(=O)[C@@H]1CCC(=O)N1 |r|
Show InChI InChI=1S/C16H20Cl2N6O4/c17-12-8(22-16(18)23-12)6-9(21-14(27)7-3-4-11(25)20-7)15(28)24-5-1-2-10(24)13(19)26/h7,9-10H,1-6H2,(H2,19,26)(H,20,25)(H,21,27)(H,22,23)/t7-,9-,10-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 5.97E+3n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay


Eur J Med Chem 111: 72-83 (2016)


Article DOI: 10.1016/j.ejmech.2016.01.038
BindingDB Entry DOI: 10.7270/Q28G8NKF
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50109023
PNG
(CHEMBL3601786)
Show SMILES CCn1c(I)nc(C[C@H](NC(=O)c2cnccn2)C(=O)N2CCC[C@H]2C(N)=O)c1I |r|
Show InChI InChI=1S/C18H21I2N7O3/c1-2-26-14(19)10(25-18(26)20)8-11(24-16(29)12-9-22-5-6-23-12)17(30)27-7-3-4-13(27)15(21)28/h5-6,9,11,13H,2-4,7-8H2,1H3,(H2,21,28)(H,24,29)/t11-,13-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 7.21E+3n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method


Bioorg Med Chem 23: 5641-53 (2015)


Article DOI: 10.1016/j.bmc.2015.07.022
BindingDB Entry DOI: 10.7270/Q2JH3NZ9
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50109018
PNG
(CHEMBL3601784)
Show SMILES NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(I)[nH]c1I)NC(=O)c1cnccn1 |r|
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 1.13E+4n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method


Bioorg Med Chem 23: 5641-53 (2015)


Article DOI: 10.1016/j.bmc.2015.07.022
BindingDB Entry DOI: 10.7270/Q2JH3NZ9
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50158397
PNG
(CHEMBL3780836)
Show SMILES NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(Cl)[nH]c1Cl)NC(=O)[C@@H]1CCC(=O)N1 |r|
Show InChI InChI=1S/C16H20Cl2N6O4/c17-12-8(22-16(18)23-12)6-9(21-14(27)7-3-4-11(25)20-7)15(28)24-5-1-2-10(24)13(19)26/h7,9-10H,1-6H2,(H2,19,26)(H,20,25)(H,21,27)(H,22,23)/t7-,9-,10-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 1.29E+4n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA


Eur J Med Chem 111: 72-83 (2016)


Article DOI: 10.1016/j.ejmech.2016.01.038
BindingDB Entry DOI: 10.7270/Q28G8NKF
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50158531
PNG
(CHEMBL3780248)
Show SMILES NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cn(Cc2ccccc2)c(Cl)n1)NC(=O)[C@@H]1CCC(=O)N1 |r|
Show InChI InChI=1S/C23H27ClN6O4/c24-23-26-15(13-29(23)12-14-5-2-1-3-6-14)11-17(28-21(33)16-8-9-19(31)27-16)22(34)30-10-4-7-18(30)20(25)32/h1-3,5-6,13,16-18H,4,7-12H2,(H2,25,32)(H,27,31)(H,28,33)/t16-,17-,18-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 1.57E+4n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA


Eur J Med Chem 111: 72-83 (2016)


Article DOI: 10.1016/j.ejmech.2016.01.038
BindingDB Entry DOI: 10.7270/Q28G8NKF
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50072397
PNG
(7-cyclohexyl-6-(2,6-dioxo-1,7-diazaspiro[4.4]non-7...)
Show SMILES NC(=O)[C@@H]1CC[C@@H]2CC(C3CCCCC3)=C(N3CC[C@]4(CCC(=O)N4)C3=O)C(=O)N12 |t:15|
Show InChI InChI=1S/C22H30N4O4/c23-19(28)16-7-6-14-12-15(13-4-2-1-3-5-13)18(20(29)26(14)16)25-11-10-22(21(25)30)9-8-17(27)24-22/h13-14,16H,1-12H2,(H2,23,28)(H,24,27)/t14-,16+,22-/m1/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 1.80E+4n/an/an/an/a



Washington University

Curated by ChEMBL


Assay Description
Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.


Bioorg Med Chem Lett 8: 3093-6 (1999)


Article DOI: 10.1016/S0960-894X(98)00567-8
BindingDB Entry DOI: 10.7270/Q21R6PP1
More data for this
Ligand-Target Pair
Thyrotropin-releasing hormone receptor


(MOUSE)
BDBM50109036
PNG
(CHEMBL3600451)
Show SMILES NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc[nH]c1Cl)NC(=O)c1cnccn1 |r|
Show InChI InChI=1S/C16H18ClN7O3/c17-13-9(21-8-22-13)6-10(23-15(26)11-7-19-3-4-20-11)16(27)24-5-1-2-12(24)14(18)25/h3-4,7-8,10,12H,1-2,5-6H2,(H2,18,25)(H,21,22)(H,23,26)/t10-,12-/m0/s1
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/an/an/a 1.94E+4n/an/an/an/a



National Institute of Pharmaceutical Education and Research

Curated by ChEMBL


Assay Description
Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method


Bioorg Med Chem 23: 5641-53 (2015)


Article DOI: 10.1016/j.bmc.2015.07.022
BindingDB Entry DOI: 10.7270/Q2JH3NZ9
More data for this
Ligand-Target Pair
Displayed 1 to 50 (of 57 total )  |  Next  |  Last  >>
Jump to: