BDBM50072394 1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyrrolylcarboxamido)propanoyl]tetrahydro-1H-2-pyrrolecarboxamide::A-38579::ABBOTT-38579::PROTIRELIN
SMILES: NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1
InChI Key: InChIKey=XNSAINXGIQZQOO-SRVKXCTJSA-N
Target/Host (Institution) | Ligand | Target/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 | pH | Temp °C |
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Thyrotropin-releasing hormone receptor 2 (Rattus norvegicus) | BDBM50072394 (1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...) | KEGG UniProtKB/TrEMBL GoogleScholar AffyNet | Purchase KEGG PC cid PC sid UniChem Similars | Article PubMed | 10 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
National Institute of Pharmaceutical Education and Research Curated by ChEMBL | Assay Description Displacement of [3H]N(1)-Me-His-TRH from TRHR2 | Bioorg Med Chem 15: 433-43 (2006) Article DOI: 10.1016/j.bmc.2006.09.045 BindingDB Entry DOI: 10.7270/Q2ZW1KJV | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Thyrotropin-releasing hormone receptor 2 (Rattus norvegicus) | BDBM50072394 (1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...) | KEGG UniProtKB/TrEMBL GoogleScholar AffyNet | Purchase KEGG PC cid PC sid UniChem Similars | Article PubMed | 10 | n/a | n/a | n/a | n/a | n/a | n/a | 7.4 | n/a |
National Institute of Pharmaceutical Education and Research Curated by ChEMBL | Assay Description Inhibitory constant against thyrotropin releasing hormone receptor 2 expressed in HEK 293EM cells upon incubation at 37 degee C for 1 hr at pH 7.4 us... | J Med Chem 48: 6162-5 (2005) Article DOI: 10.1021/jm0505462 BindingDB Entry DOI: 10.7270/Q2PK0FQG | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Thyrotropin-releasing hormone receptor (MOUSE) | BDBM50072394 (1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...) | Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL GoogleScholar AffyNet | Purchase KEGG PC cid PC sid UniChem Similars | Article PubMed | 10 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Washington University Curated by ChEMBL | Assay Description Binding affinity against 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 (Homo sapiens (Human)) | BDBM50072394 (1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...) | Reactome pathway KEGG UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase KEGG PC cid PC sid UniChem Similars | Article PubMed | 20 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
National Institute of Pharmaceutical Education and Research Curated by ChEMBL | Assay Description Displacement of [3H]N(1)-Me-His-TRH from TRHR1 | Bioorg Med Chem 15: 433-43 (2006) Article DOI: 10.1016/j.bmc.2006.09.045 BindingDB Entry DOI: 10.7270/Q2ZW1KJV | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Thyrotropin-releasing hormone receptor (Rattus norvegicus) | BDBM50072394 (1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...) | KEGG UniProtKB/SwissProt GoogleScholar AffyNet | Purchase KEGG PC cid PC sid UniChem Similars | Article PubMed | 20 | n/a | n/a | n/a | n/a | n/a | n/a | 7.4 | n/a |
National Institute of Pharmaceutical Education and Research Curated by ChEMBL | Assay Description Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degee C for 1 hr at pH 7.4 us... | J Med Chem 48: 6162-5 (2005) Article DOI: 10.1021/jm0505462 BindingDB Entry DOI: 10.7270/Q2PK0FQG | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Thyrotropin-releasing hormone receptor (MOUSE) | BDBM50072394 (1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...) | Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL GoogleScholar AffyNet | Purchase KEGG PC cid PC sid UniChem Similars | Article PubMed | 23 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/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 (Rattus norvegicus) | BDBM50072394 (1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...) | KEGG UniProtKB/SwissProt GoogleScholar AffyNet | Purchase KEGG PC cid PC sid UniChem Similars | Article PubMed | 42 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
University of Florida Curated by ChEMBL | Assay Description Inhibition of [3H]-[3-Me-His2]-TRH binding to thyrotropin releasing hormone receptor of rat forebrain | J Med Chem 47: 6025-33 (2004) Article DOI: 10.1021/jm020531t BindingDB Entry DOI: 10.7270/Q2W095F0 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Thyrotropin-releasing hormone receptor 2 (Rattus norvegicus) | BDBM50072394 (1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...) | KEGG UniProtKB/TrEMBL GoogleScholar AffyNet | Purchase KEGG PC cid PC sid UniChem Similars | Article PubMed | n/a | n/a | 23 | n/a | n/a | n/a | n/a | n/a | n/a |
Griffith University Curated by ChEMBL | Assay Description Displacement of [3H]3-methylhistidyl-TRH from rat recombinant TRHR2 expressed in HEK2935 cells | J Nat Prod 71: 884-6 (2008) Article DOI: 10.1021/np070658r BindingDB Entry DOI: 10.7270/Q2MC8ZTC | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Thyrotropin-releasing hormone receptor 2 (Rattus norvegicus) | BDBM50072394 (1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...) | KEGG UniProtKB/TrEMBL GoogleScholar AffyNet | Purchase KEGG PC cid PC sid UniChem Similars | Article PubMed | n/a | n/a | 2.30E+4 | n/a | n/a | n/a | n/a | n/a | n/a |
Griffith University Curated by ChEMBL | Assay Description Displacement of [3H]3-methylhistidyl-TRH from rat recombinant TRH2 receptor expressed in HEK2935 cells | J Nat Prod 71: 881-3 (2008) Article DOI: 10.1021/np0706567 BindingDB Entry DOI: 10.7270/Q2ZK5GFP | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Thyrotropin-releasing hormone receptor (MOUSE) | BDBM50072394 (1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...) | Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL GoogleScholar AffyNet | Purchase KEGG PC cid PC sid UniChem Similars | PubMed | n/a | n/a | n/a | n/a | 3.20 | n/a | n/a | n/a | n/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) BindingDB Entry DOI: 10.7270/Q28G8NKF | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Thyrotropin-releasing hormone receptor 2 (Mus musculus) | BDBM50072394 (1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...) | UniProtKB/TrEMBL GoogleScholar AffyNet | Purchase KEGG PC cid PC sid UniChem Similars | PubMed | n/a | n/a | 7 | n/a | n/a | n/a | n/a | n/a | n/a |
National Institute of Pharmaceutical Education and Research Curated by ChEMBL | Assay Description Displacement of [3H]-Me-His-TRH from mouse TRH-R2 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs | Eur J Med Chem 111: 72-83 (2016) BindingDB Entry DOI: 10.7270/Q28G8NKF | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Thyrotropin-releasing hormone receptor (MOUSE) | BDBM50072394 (1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...) | Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL GoogleScholar AffyNet | Purchase KEGG PC cid PC sid UniChem Similars | PubMed | n/a | n/a | n/a | n/a | 1 | n/a | n/a | n/a | n/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) BindingDB Entry DOI: 10.7270/Q28G8NKF | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Thyrotropin-releasing hormone receptor 2 (Mus musculus) | BDBM50072394 (1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...) | UniProtKB/TrEMBL GoogleScholar AffyNet | Purchase KEGG PC cid PC sid UniChem Similars | PubMed | n/a | n/a | n/a | n/a | 0.5 | n/a | n/a | n/a | n/a |
National Institute of Pharmaceutical Education and Research Curated by ChEMBL | Assay Description Agonist activity at mouse TRH-R2 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay | Eur J Med Chem 111: 72-83 (2016) BindingDB Entry DOI: 10.7270/Q28G8NKF | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Thyrotropin-releasing hormone receptor (MOUSE) | BDBM50072394 (1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...) | Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL GoogleScholar AffyNet | Purchase KEGG PC cid PC sid UniChem Similars | PubMed | n/a | n/a | 26 | n/a | n/a | n/a | n/a | n/a | n/a |
National Institute of Pharmaceutical Education and Research Curated by ChEMBL | Assay Description Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs | Eur J Med Chem 111: 72-83 (2016) BindingDB Entry DOI: 10.7270/Q28G8NKF | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Thyrotropin-releasing hormone receptor 2 (Mus musculus) | BDBM50072394 (1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...) | UniProtKB/TrEMBL GoogleScholar AffyNet | Purchase KEGG PC cid PC sid UniChem Similars | PubMed | n/a | n/a | n/a | n/a | 3.10 | n/a | n/a | n/a | n/a |
National Institute of Pharmaceutical Education and Research Curated by ChEMBL | Assay Description Agonist activity at mouse TRH-R2 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA | Eur J Med Chem 111: 72-83 (2016) BindingDB Entry DOI: 10.7270/Q28G8NKF | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Thyrotropin-releasing hormone receptor (MOUSE) | BDBM50072394 (1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...) | Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL GoogleScholar AffyNet | Purchase KEGG PC cid PC sid UniChem Similars | Article PubMed | n/a | n/a | n/a | n/a | 0.490 | n/a | n/a | n/a | n/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 (1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...) | Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL GoogleScholar AffyNet | Purchase KEGG PC cid PC sid UniChem Similars | Article PubMed | n/a | n/a | n/a | n/a | 0.680 | n/a | n/a | n/a | n/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 2 (Mus musculus) | BDBM50072394 (1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...) | UniProtKB/TrEMBL GoogleScholar AffyNet | Purchase KEGG PC cid PC sid UniChem Similars | PubMed | n/a | n/a | n/a | n/a | 0.520 | n/a | n/a | n/a | n/a |
National Institute of Pharmaceutical Education and Research Curated by ChEMBL | Assay Description Agonist activity at mouse TRH-R2 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method | Bioorg Med Chem 23: 5641-53 (2015) BindingDB Entry DOI: 10.7270/Q2JH3NZ9 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Thyrotropin-releasing hormone receptor (MOUSE) | BDBM50072394 (1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...) | Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL GoogleScholar AffyNet | Purchase KEGG PC cid PC sid UniChem Similars | PubMed | n/a | n/a | 2.60 | n/a | n/a | n/a | n/a | n/a | n/a |
National Institute of Pharmaceutical Education and Research Curated by ChEMBL | Assay Description Displacement of [3H]-1-MeHis-TRH from mouse TRH-R1 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting method | Bioorg Med Chem 23: 5641-53 (2015) BindingDB Entry DOI: 10.7270/Q2JH3NZ9 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Thyrotropin-releasing hormone receptor 2 (Mus musculus) | BDBM50072394 (1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...) | UniProtKB/TrEMBL GoogleScholar AffyNet | Purchase KEGG PC cid PC sid UniChem Similars | PubMed | n/a | n/a | 7 | n/a | n/a | n/a | n/a | n/a | n/a |
National Institute of Pharmaceutical Education and Research Curated by ChEMBL | Assay Description Displacement of [3H]-1-MeHis-TRH from mouse TRH-R2 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting method | Bioorg Med Chem 23: 5641-53 (2015) BindingDB Entry DOI: 10.7270/Q2JH3NZ9 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Thyrotropin-releasing hormone receptor 2 (Rattus norvegicus) | BDBM50072394 (1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...) | KEGG UniProtKB/TrEMBL GoogleScholar AffyNet | Purchase KEGG PC cid PC sid UniChem Similars | Article PubMed | n/a | n/a | n/a | n/a | 3 | n/a | n/a | n/a | n/a |
National Institute of Pharmaceutical Education and Research Curated by ChEMBL | Assay Description Agonist activity at TRHR2 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activity | Bioorg Med Chem 15: 433-43 (2006) Article DOI: 10.1016/j.bmc.2006.09.045 BindingDB Entry DOI: 10.7270/Q2ZW1KJV | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Thyrotropin-releasing hormone receptor (Homo sapiens (Human)) | BDBM50072394 (1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...) | Reactome pathway KEGG UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase KEGG PC cid PC sid UniChem Similars | Article PubMed | n/a | n/a | n/a | n/a | 3 | n/a | n/a | n/a | n/a |
National Institute of Pharmaceutical Education and Research Curated by ChEMBL | Assay Description Agonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activity | Bioorg Med Chem 15: 433-43 (2006) Article DOI: 10.1016/j.bmc.2006.09.045 BindingDB Entry DOI: 10.7270/Q2ZW1KJV | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Thyrotropin-releasing hormone receptor 2 (Rattus norvegicus) | BDBM50072394 (1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...) | KEGG UniProtKB/TrEMBL GoogleScholar AffyNet | Purchase KEGG PC cid PC sid UniChem Similars | Article PubMed | n/a | n/a | n/a | n/a | 3 | n/a | n/a | 7.8 | n/a |
National Institute of Pharmaceutical Education and Research Curated by ChEMBL | Assay Description Signaling (activation) potency for thyrotropin releasing hormone receptor 2 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubatio... | J Med Chem 48: 6162-5 (2005) Article DOI: 10.1021/jm0505462 BindingDB Entry DOI: 10.7270/Q2PK0FQG | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Thyrotropin-releasing hormone receptor (Rattus norvegicus) | BDBM50072394 (1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...) | KEGG UniProtKB/SwissProt GoogleScholar AffyNet | Purchase KEGG PC cid PC sid UniChem Similars | Article PubMed | n/a | n/a | n/a | n/a | 3 | n/a | n/a | 7.8 | n/a |
National Institute of Pharmaceutical Education and Research Curated by ChEMBL | Assay Description Signaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubatio... | J Med Chem 48: 6162-5 (2005) Article DOI: 10.1021/jm0505462 BindingDB Entry DOI: 10.7270/Q2PK0FQG | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Thyrotropin-releasing hormone receptor (MOUSE) | BDBM50072394 (1-[3-(1H-4-imidazolyl)-2-(5-oxotetrahydro-1H-2-pyr...) | Reactome pathway KEGG UniProtKB/SwissProt UniProtKB/TrEMBL GoogleScholar AffyNet | Purchase KEGG PC cid PC sid UniChem Similars | PubMed | n/a | n/a | n/a | n/a | 1 | n/a | n/a | n/a | n/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) BindingDB Entry DOI: 10.7270/Q2JH3NZ9 | |||||||||||
More data for this Ligand-Target Pair |