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Compile Data Set for Download or QSAR

Found 491 hits with Last Name = 'yano' and Initial = 't'   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kJ/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50234480
PNG
(CHEMBL4069551)
Show SMILES CCC(CC)c1ccc(Cl)c2nc(Oc3c(C)cc(Cl)cc3Cl)n(C)c12
Show InChI InChI=1S/C20H21Cl3N2O/c1-5-12(6-2)14-7-8-15(22)17-18(14)25(4)20(24-17)26-19-11(3)9-13(21)10-16(19)23/h7-10,12H,5-6H2,1-4H3
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n/an/a 4.10n/an/an/an/an/an/a



Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition meas...


Bioorg Med Chem 25: 1556-1570 (2017)


Article DOI: 10.1016/j.bmc.2016.11.011
BindingDB Entry DOI: 10.7270/Q23R0W4P
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50460165
PNG
(CHEMBL4225254)
Show SMILES CCN(CC)c1ccc(Cl)c2nc3N(CCCn3c12)c1ccc(Cl)cc1Cl
Show InChI InChI=1S/C20H21Cl3N4/c1-3-25(4-2)17-9-7-14(22)18-19(17)27-11-5-10-26(20(27)24-18)16-8-6-13(21)12-15(16)23/h6-9,12H,3-5,10-11H2,1-2H3
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n/an/a 4.40n/an/an/an/an/an/a



Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Antagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of human CRF-stimulated cAMP accumulation after 4 hrs by luc...


Bioorg Med Chem 26: 2229-2250 (2018)


Article DOI: 10.1016/j.bmc.2018.01.020
BindingDB Entry DOI: 10.7270/Q2474DG1
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50460165
PNG
(CHEMBL4225254)
Show SMILES CCN(CC)c1ccc(Cl)c2nc3N(CCCn3c12)c1ccc(Cl)cc1Cl
Show InChI InChI=1S/C20H21Cl3N4/c1-3-25(4-2)17-9-7-14(22)18-19(17)27-11-5-10-26(20(27)24-18)16-8-6-13(21)12-15(16)23/h6-9,12H,3-5,10-11H2,1-2H3
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n/an/a 7.10n/an/an/an/an/an/a



Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method


Bioorg Med Chem 26: 2229-2250 (2018)


Article DOI: 10.1016/j.bmc.2018.01.020
BindingDB Entry DOI: 10.7270/Q2474DG1
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50234477
PNG
(CHEMBL4087369)
Show SMILES CCCC(CCC)c1ccc(Cl)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12
Show InChI InChI=1S/C23H29Cl2N3O/c1-6-8-15(9-7-2)17-10-11-18(25)21-22(17)28(4)23(27-21)26-20-14(3)12-16(24)13-19(20)29-5/h10-13,15H,6-9H2,1-5H3,(H,26,27)
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n/an/a 7.40n/an/an/an/an/an/a



Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition meas...


Bioorg Med Chem 25: 1556-1570 (2017)


Article DOI: 10.1016/j.bmc.2016.11.011
BindingDB Entry DOI: 10.7270/Q23R0W4P
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50161874
PNG
(CHEMBL3794475)
Show SMILES CCN(CC)c1ccc(C)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12
Show InChI InChI=1S/C21H27ClN4O/c1-7-26(8-2)16-10-9-13(3)19-20(16)25(5)21(24-19)23-18-14(4)11-15(22)12-17(18)27-6/h9-12H,7-8H2,1-6H3,(H,23,24)
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n/an/a 7.60n/an/an/an/an/an/a



Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method


J Med Chem 59: 2551-66 (2016)


Article DOI: 10.1021/acs.jmedchem.5b01715
BindingDB Entry DOI: 10.7270/Q24F1SNR
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50234487
PNG
(CHEMBL4070898)
Show SMILES CCC(CC)c1ccc(Cl)c2nc(Nc3c(C)cc(Cl)cc3Cl)n(C)c12
Show InChI InChI=1S/C20H22Cl3N3/c1-5-12(6-2)14-7-8-15(22)18-19(14)26(4)20(25-18)24-17-11(3)9-13(21)10-16(17)23/h7-10,12H,5-6H2,1-4H3,(H,24,25)
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n/an/a 7.90n/an/an/an/an/an/a



Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method


Bioorg Med Chem 25: 1556-1570 (2017)


Article DOI: 10.1016/j.bmc.2016.11.011
BindingDB Entry DOI: 10.7270/Q23R0W4P
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50116105
PNG
(3-(6-(dimethylamino)-4-methylpyridin-3-yl)-2,5-dim...)
Show SMILES CCCN(CCC)c1cc(C)nc2c(c(C)nn12)-c1cnc(cc1C)N(C)C |(-1.91,-13.39,;-3.24,-14.16,;-4.58,-13.4,;-5.91,-14.18,;-7.24,-13.41,;-8.57,-14.19,;-9.91,-13.42,;-5.9,-15.72,;-7.22,-16.49,;-7.23,-18.03,;-8.56,-18.8,;-5.9,-18.8,;-4.55,-18.03,;-3.07,-18.5,;-2.16,-17.24,;-.62,-17.23,;-3.09,-15.99,;-4.56,-16.48,;-2.58,-19.96,;-3.61,-21.11,;-3.13,-22.57,;-1.62,-22.88,;-.59,-21.72,;-1.08,-20.27,;-.06,-19.11,;-1.13,-24.34,;.38,-24.65,;-2.15,-25.5,)|
Show InChI InChI=1S/C22H32N6/c1-8-10-27(11-9-2)20-13-16(4)24-22-21(17(5)25-28(20)22)18-14-23-19(26(6)7)12-15(18)3/h12-14H,8-11H2,1-7H3
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n/an/a 8.5n/an/an/an/an/an/a



Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method


J Med Chem 59: 2551-66 (2016)


Article DOI: 10.1021/acs.jmedchem.5b01715
BindingDB Entry DOI: 10.7270/Q24F1SNR
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50234482
PNG
(CHEMBL4096045)
Show SMILES CCC(CC)c1ccc(Cl)c2nc(Oc3c(C)cc(cc3Cl)C#N)n(C)c12
Show InChI InChI=1S/C21H21Cl2N3O/c1-5-14(6-2)15-7-8-16(22)18-19(15)26(4)21(25-18)27-20-12(3)9-13(11-24)10-17(20)23/h7-10,14H,5-6H2,1-4H3
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n/an/a 8.60n/an/an/an/an/an/a



Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition meas...


Bioorg Med Chem 25: 1556-1570 (2017)


Article DOI: 10.1016/j.bmc.2016.11.011
BindingDB Entry DOI: 10.7270/Q23R0W4P
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50161867
PNG
(CHEMBL3793277)
Show SMILES CCN(CC)c1ccc(Cl)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12
Show InChI InChI=1S/C20H24Cl2N4O/c1-6-26(7-2)15-9-8-14(22)18-19(15)25(4)20(24-18)23-17-12(3)10-13(21)11-16(17)27-5/h8-11H,6-7H2,1-5H3,(H,23,24)
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n/an/a 9.5n/an/an/an/an/an/a



Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method


Bioorg Med Chem 26: 2229-2250 (2018)


Article DOI: 10.1016/j.bmc.2018.01.020
BindingDB Entry DOI: 10.7270/Q2474DG1
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50161832
PNG
(CHEMBL3792517)
Show SMILES CCCN(CCC)c1ccc(Cl)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12
Show InChI InChI=1S/C22H28Cl2N4O/c1-6-10-28(11-7-2)17-9-8-16(24)20-21(17)27(4)22(26-20)25-19-14(3)12-15(23)13-18(19)29-5/h8-9,12-13H,6-7,10-11H2,1-5H3,(H,25,26)
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n/an/a 9.5n/an/an/an/an/an/a



Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition meas...


Bioorg Med Chem 25: 1556-1570 (2017)


Article DOI: 10.1016/j.bmc.2016.11.011
BindingDB Entry DOI: 10.7270/Q23R0W4P
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50161832
PNG
(CHEMBL3792517)
Show SMILES CCCN(CCC)c1ccc(Cl)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12
Show InChI InChI=1S/C22H28Cl2N4O/c1-6-10-28(11-7-2)17-9-8-16(24)20-21(17)27(4)22(26-20)25-19-14(3)12-15(23)13-18(19)29-5/h8-9,12-13H,6-7,10-11H2,1-5H3,(H,25,26)
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n/an/a 9.5n/an/an/an/an/an/a



Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method


J Med Chem 59: 2551-66 (2016)


Article DOI: 10.1021/acs.jmedchem.5b01715
BindingDB Entry DOI: 10.7270/Q24F1SNR
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50161862
PNG
(CHEMBL3793568)
Show SMILES Cl.CCN(C(C)C)c1cccc2nc(Nc3c(C)cc(Br)cc3OC)n(C)c12
Show InChI InChI=1S/C21H27BrN4O.ClH/c1-7-26(13(2)3)17-10-8-9-16-20(17)25(5)21(23-16)24-19-14(4)11-15(22)12-18(19)27-6;/h8-13H,7H2,1-6H3,(H,23,24);1H
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n/an/a 11n/an/an/an/an/an/a



Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method


J Med Chem 59: 2551-66 (2016)


Article DOI: 10.1021/acs.jmedchem.5b01715
BindingDB Entry DOI: 10.7270/Q24F1SNR
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50460180
PNG
(CHEMBL4224887)
Show SMILES CCN(CC)c1cccc2nc3N(CCCn3c12)c1ccc(Cl)cc1Cl
Show InChI InChI=1S/C20H22Cl2N4/c1-3-24(4-2)18-8-5-7-16-19(18)26-12-6-11-25(20(26)23-16)17-10-9-14(21)13-15(17)22/h5,7-10,13H,3-4,6,11-12H2,1-2H3
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n/an/a 11n/an/an/an/an/an/a



Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method


Bioorg Med Chem 26: 2229-2250 (2018)


Article DOI: 10.1016/j.bmc.2018.01.020
BindingDB Entry DOI: 10.7270/Q2474DG1
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50058163
PNG
(Butyl-[2,5-dimethyl-7-(2,4,6-trimethyl-phenyl)-7H-...)
Show SMILES CCCCN(CC)c1nc(C)nc2n(cc(C)c12)-c1c(C)cc(C)cc1C |(-10.62,2.69,;-9.29,3.46,;-7.95,2.7,;-6.62,3.48,;-5.28,2.71,;-3.95,3.49,;-3.96,5.03,;-5.27,1.17,;-6.6,.4,;-6.6,-1.14,;-7.94,-1.91,;-5.27,-1.91,;-3.92,-1.14,;-2.44,-1.61,;-1.54,-.35,;-2.46,.9,;-1.99,2.37,;-3.93,.41,;-1.96,-3.07,;-2.99,-4.22,;-4.49,-3.91,;-2.5,-5.68,;-.99,-5.99,;-.51,-7.46,;.03,-4.83,;-.46,-3.38,;.56,-2.22,)|
Show InChI InChI=1S/C23H32N4/c1-8-10-11-26(9-2)22-20-18(6)14-27(23(20)25-19(7)24-22)21-16(4)12-15(3)13-17(21)5/h12-14H,8-11H2,1-7H3
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n/an/a 11n/an/an/an/an/an/a



Takeda Pharmaceutical Company Ltd

Curated by ChEMBL


Assay Description
Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells


Bioorg Med Chem Lett 21: 2365-71 (2011)


Article DOI: 10.1016/j.bmcl.2011.02.086
BindingDB Entry DOI: 10.7270/Q20Z73JB
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50161858
PNG
(CHEMBL3793367)
Show SMILES Cl.CCCN(CCC)c1cccc2nc(Nc3c(C)cc(Br)cc3OC)n(C)c12
Show InChI InChI=1S/C22H29BrN4O.ClH/c1-6-11-27(12-7-2)18-10-8-9-17-21(18)26(4)22(24-17)25-20-15(3)13-16(23)14-19(20)28-5;/h8-10,13-14H,6-7,11-12H2,1-5H3,(H,24,25);1H
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n/an/a 12n/an/an/an/an/an/a



Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method


J Med Chem 59: 2551-66 (2016)


Article DOI: 10.1021/acs.jmedchem.5b01715
BindingDB Entry DOI: 10.7270/Q24F1SNR
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50161868
PNG
(CHEMBL3793070)
Show SMILES CCN(CC)c1ccc(C#N)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12
Show InChI InChI=1S/C21H24ClN5O/c1-6-27(7-2)16-9-8-14(12-23)19-20(16)26(4)21(25-19)24-18-13(3)10-15(22)11-17(18)28-5/h8-11H,6-7H2,1-5H3,(H,24,25)
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n/an/a 13n/an/an/an/an/an/a



Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method


J Med Chem 59: 2551-66 (2016)


Article DOI: 10.1021/acs.jmedchem.5b01715
BindingDB Entry DOI: 10.7270/Q24F1SNR
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50536884
PNG
(CHEMBL4581950)
Show SMILES COc1cc(Cl)cc(C)c1Nc1nc2cccc(N(C(C)C)c3ccccc3)c2n1C
Show InChI InChI=1S/C25H27ClN4O/c1-16(2)30(19-10-7-6-8-11-19)21-13-9-12-20-24(21)29(4)25(27-20)28-23-17(3)14-18(26)15-22(23)31-5/h6-16H,1-5H3,(H,27,28)
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n/an/a 13n/an/an/an/an/an/a



Takeda Pharmaceutical Company Ltd

Curated by ChEMBL


Assay Description
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method


Bioorg Med Chem 24: 4675-4691 (2016)


Article DOI: 10.1016/j.bmc.2016.08.005
BindingDB Entry DOI: 10.7270/Q2G164BQ
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50161958
PNG
(CHEMBL3794479)
Show SMILES CCN(CC)c1ccc(OC)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12
Show InChI InChI=1S/C21H27ClN4O2/c1-7-26(8-2)15-9-10-16(27-5)19-20(15)25(4)21(24-19)23-18-13(3)11-14(22)12-17(18)28-6/h9-12H,7-8H2,1-6H3,(H,23,24)
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Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method


J Med Chem 59: 2551-66 (2016)


Article DOI: 10.1021/acs.jmedchem.5b01715
BindingDB Entry DOI: 10.7270/Q24F1SNR
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50161860
PNG
(CHEMBL3793322)
Show SMILES Cl.CCN(CC)c1cccc2nc(Nc3c(C)cc(Br)cc3OC)n(C)c12
Show InChI InChI=1S/C20H25BrN4O.ClH/c1-6-25(7-2)16-10-8-9-15-19(16)24(4)20(22-15)23-18-13(3)11-14(21)12-17(18)26-5;/h8-12H,6-7H2,1-5H3,(H,22,23);1H
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Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method


J Med Chem 59: 2551-66 (2016)


Article DOI: 10.1021/acs.jmedchem.5b01715
BindingDB Entry DOI: 10.7270/Q24F1SNR
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50161861
PNG
(CHEMBL3792935)
Show SMILES Cl.CCCCN(CCCC)c1cccc2nc(Nc3c(C)cc(Br)cc3OC)n(C)c12
Show InChI InChI=1S/C24H33BrN4O.ClH/c1-6-8-13-29(14-9-7-2)20-12-10-11-19-23(20)28(4)24(26-19)27-22-17(3)15-18(25)16-21(22)30-5;/h10-12,15-16H,6-9,13-14H2,1-5H3,(H,26,27);1H
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Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method


J Med Chem 59: 2551-66 (2016)


Article DOI: 10.1021/acs.jmedchem.5b01715
BindingDB Entry DOI: 10.7270/Q24F1SNR
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50161841
PNG
(CHEMBL3793985)
Show SMILES CCCN(CCC)c1cccc2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12
Show InChI InChI=1S/C22H29ClN4O/c1-6-11-27(12-7-2)18-10-8-9-17-21(18)26(4)22(24-17)25-20-15(3)13-16(23)14-19(20)28-5/h8-10,13-14H,6-7,11-12H2,1-5H3,(H,24,25)
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Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method


J Med Chem 59: 2551-66 (2016)


Article DOI: 10.1021/acs.jmedchem.5b01715
BindingDB Entry DOI: 10.7270/Q24F1SNR
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50161866
PNG
(CHEMBL3794030)
Show SMILES CCCN(CCC)c1ccc(C#N)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12
Show InChI InChI=1S/C23H28ClN5O/c1-6-10-29(11-7-2)18-9-8-16(14-25)21-22(18)28(4)23(27-21)26-20-15(3)12-17(24)13-19(20)30-5/h8-9,12-13H,6-7,10-11H2,1-5H3,(H,26,27)
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Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method


J Med Chem 59: 2551-66 (2016)


Article DOI: 10.1021/acs.jmedchem.5b01715
BindingDB Entry DOI: 10.7270/Q24F1SNR
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50234478
PNG
(CHEMBL4101653)
Show SMILES CCC(CC)c1ccc(Cl)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12
Show InChI InChI=1S/C21H25Cl2N3O/c1-6-13(7-2)15-8-9-16(23)19-20(15)26(4)21(25-19)24-18-12(3)10-14(22)11-17(18)27-5/h8-11,13H,6-7H2,1-5H3,(H,24,25)
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Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition meas...


Bioorg Med Chem 25: 1556-1570 (2017)


Article DOI: 10.1016/j.bmc.2016.11.011
BindingDB Entry DOI: 10.7270/Q23R0W4P
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50161854
PNG
(CHEMBL3794051)
Show SMILES CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)n(C)c12
Show InChI InChI=1S/C23H32N4/c1-7-12-27(13-8-2)20-11-9-10-19-22(20)26(6)23(24-19)25-21-17(4)14-16(3)15-18(21)5/h9-11,14-15H,7-8,12-13H2,1-6H3,(H,24,25)
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Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method


J Med Chem 59: 2551-66 (2016)


Article DOI: 10.1021/acs.jmedchem.5b01715
BindingDB Entry DOI: 10.7270/Q24F1SNR
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50116105
PNG
(3-(6-(dimethylamino)-4-methylpyridin-3-yl)-2,5-dim...)
Show SMILES CCCN(CCC)c1cc(C)nc2c(c(C)nn12)-c1cnc(cc1C)N(C)C |(-1.91,-13.39,;-3.24,-14.16,;-4.58,-13.4,;-5.91,-14.18,;-7.24,-13.41,;-8.57,-14.19,;-9.91,-13.42,;-5.9,-15.72,;-7.22,-16.49,;-7.23,-18.03,;-8.56,-18.8,;-5.9,-18.8,;-4.55,-18.03,;-3.07,-18.5,;-2.16,-17.24,;-.62,-17.23,;-3.09,-15.99,;-4.56,-16.48,;-2.58,-19.96,;-3.61,-21.11,;-3.13,-22.57,;-1.62,-22.88,;-.59,-21.72,;-1.08,-20.27,;-.06,-19.11,;-1.13,-24.34,;.38,-24.65,;-2.15,-25.5,)|
Show InChI InChI=1S/C22H32N6/c1-8-10-27(11-9-2)20-13-16(4)24-22-21(17(5)25-28(20)22)18-14-23-19(26(6)7)12-15(18)3/h12-14H,8-11H2,1-7H3
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Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition meas...


Bioorg Med Chem 25: 1556-1570 (2017)


Article DOI: 10.1016/j.bmc.2016.11.011
BindingDB Entry DOI: 10.7270/Q23R0W4P
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50234484
PNG
(CHEMBL4070523)
Show SMILES CCN(CCC(F)(F)F)c1ccc(Br)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12
Show InChI InChI=1S/C21H23BrClF3N4O/c1-5-30(9-8-21(24,25)26)15-7-6-14(22)18-19(15)29(3)20(28-18)27-17-12(2)10-13(23)11-16(17)31-4/h6-7,10-11H,5,8-9H2,1-4H3,(H,27,28)
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Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition meas...


Bioorg Med Chem 25: 1556-1570 (2017)


Article DOI: 10.1016/j.bmc.2016.11.011
BindingDB Entry DOI: 10.7270/Q23R0W4P
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50460172
PNG
(CHEMBL4225516)
Show SMILES CCN(CC)c1cccc2nc(Nc3c(C)cc(Cl)cc3Cl)n(C)c12
Show InChI InChI=1S/C19H22Cl2N4/c1-5-25(6-2)16-9-7-8-15-18(16)24(4)19(22-15)23-17-12(3)10-13(20)11-14(17)21/h7-11H,5-6H2,1-4H3,(H,22,23)
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Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method


Bioorg Med Chem 26: 2229-2250 (2018)


Article DOI: 10.1016/j.bmc.2018.01.020
BindingDB Entry DOI: 10.7270/Q2474DG1
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50460167
PNG
(CHEMBL4225316)
Show SMILES CCC(OC)c1ccc(Cl)c2nc3N(CCCn3c12)c1ccc(Cl)cc1Cl
Show InChI InChI=1S/C20H20Cl3N3O/c1-3-17(27-2)13-6-7-14(22)18-19(13)26-10-4-9-25(20(26)24-18)16-8-5-12(21)11-15(16)23/h5-8,11,17H,3-4,9-10H2,1-2H3
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Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method


Bioorg Med Chem 26: 2229-2250 (2018)


Article DOI: 10.1016/j.bmc.2018.01.020
BindingDB Entry DOI: 10.7270/Q2474DG1
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50161859
PNG
(CHEMBL3792636)
Show SMILES Cl.CCCN(CCC)c1cccc2nc(Nc3c(C)cc(Cl)cc3C(C)C)n(C)c12
Show InChI InChI=1S/C24H33ClN4.ClH/c1-7-12-29(13-8-2)21-11-9-10-20-23(21)28(6)24(26-20)27-22-17(5)14-18(25)15-19(22)16(3)4;/h9-11,14-16H,7-8,12-13H2,1-6H3,(H,26,27);1H
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Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method


J Med Chem 59: 2551-66 (2016)


Article DOI: 10.1021/acs.jmedchem.5b01715
BindingDB Entry DOI: 10.7270/Q24F1SNR
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50234483
PNG
(CHEMBL4068170)
Show SMILES CCC(CC)c1ccc(Cl)c2nc(Oc3c(C)cc(cc3Cl)C(N)=O)n(C)c12
Show InChI InChI=1S/C21H23Cl2N3O2/c1-5-12(6-2)14-7-8-15(22)17-18(14)26(4)21(25-17)28-19-11(3)9-13(20(24)27)10-16(19)23/h7-10,12H,5-6H2,1-4H3,(H2,24,27)
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Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition meas...


Bioorg Med Chem 25: 1556-1570 (2017)


Article DOI: 10.1016/j.bmc.2016.11.011
BindingDB Entry DOI: 10.7270/Q23R0W4P
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50234480
PNG
(CHEMBL4069551)
Show SMILES CCC(CC)c1ccc(Cl)c2nc(Oc3c(C)cc(Cl)cc3Cl)n(C)c12
Show InChI InChI=1S/C20H21Cl3N2O/c1-5-12(6-2)14-7-8-15(22)17-18(14)25(4)20(24-17)26-19-11(3)9-13(21)10-16(19)23/h7-10,12H,5-6H2,1-4H3
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Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition meas...


Bioorg Med Chem 25: 1556-1570 (2017)


Article DOI: 10.1016/j.bmc.2016.11.011
BindingDB Entry DOI: 10.7270/Q23R0W4P
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50161867
PNG
(CHEMBL3793277)
Show SMILES CCN(CC)c1ccc(Cl)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12
Show InChI InChI=1S/C20H24Cl2N4O/c1-6-26(7-2)15-9-8-14(22)18-19(15)25(4)20(24-18)23-17-12(3)10-13(21)11-16(17)27-5/h8-11H,6-7H2,1-5H3,(H,23,24)
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Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method


J Med Chem 59: 2551-66 (2016)


Article DOI: 10.1021/acs.jmedchem.5b01715
BindingDB Entry DOI: 10.7270/Q24F1SNR
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50161867
PNG
(CHEMBL3793277)
Show SMILES CCN(CC)c1ccc(Cl)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12
Show InChI InChI=1S/C20H24Cl2N4O/c1-6-26(7-2)15-9-8-14(22)18-19(15)25(4)20(24-18)23-17-12(3)10-13(21)11-16(17)27-5/h8-11H,6-7H2,1-5H3,(H,23,24)
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Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition meas...


Bioorg Med Chem 25: 1556-1570 (2017)


Article DOI: 10.1016/j.bmc.2016.11.011
BindingDB Entry DOI: 10.7270/Q23R0W4P
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50536887
PNG
(CHEMBL4591335)
Show SMILES COc1cc(Cl)cc(C)c1Nc1nc2cccc(N(C(C)C)c3ccc(Cl)cc3)c2n1C
Show InChI InChI=1S/C25H26Cl2N4O/c1-15(2)31(19-11-9-17(26)10-12-19)21-8-6-7-20-24(21)30(4)25(28-20)29-23-16(3)13-18(27)14-22(23)32-5/h6-15H,1-5H3,(H,28,29)
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Takeda Pharmaceutical Company Ltd

Curated by ChEMBL


Assay Description
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method


Bioorg Med Chem 24: 4675-4691 (2016)


Article DOI: 10.1016/j.bmc.2016.08.005
BindingDB Entry DOI: 10.7270/Q2G164BQ
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50536892
PNG
(CHEMBL4544244)
Show SMILES COc1ccc(cn1)N(C(C)C)c1cccc2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12
Show InChI InChI=1S/C25H28ClN5O2/c1-15(2)31(18-10-11-22(33-6)27-14-18)20-9-7-8-19-24(20)30(4)25(28-19)29-23-16(3)12-17(26)13-21(23)32-5/h7-15H,1-6H3,(H,28,29)
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Takeda Pharmaceutical Company Ltd

Curated by ChEMBL


Assay Description
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method


Bioorg Med Chem 24: 4675-4691 (2016)


Article DOI: 10.1016/j.bmc.2016.08.005
BindingDB Entry DOI: 10.7270/Q2G164BQ
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50536883
PNG
(CHEMBL4593848)
Show SMILES COc1ccc(cc1)N(C(C)C)c1cccc2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12
Show InChI InChI=1S/C26H29ClN4O2/c1-16(2)31(19-10-12-20(32-5)13-11-19)22-9-7-8-21-25(22)30(4)26(28-21)29-24-17(3)14-18(27)15-23(24)33-6/h7-16H,1-6H3,(H,28,29)
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Takeda Pharmaceutical Company Ltd

Curated by ChEMBL


Assay Description
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method


Bioorg Med Chem 24: 4675-4691 (2016)


Article DOI: 10.1016/j.bmc.2016.08.005
BindingDB Entry DOI: 10.7270/Q2G164BQ
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50234480
PNG
(CHEMBL4069551)
Show SMILES CCC(CC)c1ccc(Cl)c2nc(Oc3c(C)cc(Cl)cc3Cl)n(C)c12
Show InChI InChI=1S/C20H21Cl3N2O/c1-5-12(6-2)14-7-8-15(22)17-18(14)25(4)20(24-17)26-19-11(3)9-13(21)10-16(19)23/h7-10,12H,5-6H2,1-4H3
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n/an/a 32n/an/an/an/an/an/a



Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by compound washout for 2 h...


Bioorg Med Chem 25: 1556-1570 (2017)


Article DOI: 10.1016/j.bmc.2016.11.011
BindingDB Entry DOI: 10.7270/Q23R0W4P
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50460183
PNG
(CHEMBL4227554)
Show SMILES CCN(CC)c1cccc2nc3C(CCCn3c12)c1ccc(Cl)cc1Cl
Show InChI InChI=1S/C21H23Cl2N3/c1-3-25(4-2)19-9-5-8-18-20(19)26-12-6-7-16(21(26)24-18)15-11-10-14(22)13-17(15)23/h5,8-11,13,16H,3-4,6-7,12H2,1-2H3
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Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method


Bioorg Med Chem 26: 2229-2250 (2018)


Article DOI: 10.1016/j.bmc.2018.01.020
BindingDB Entry DOI: 10.7270/Q2474DG1
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50460170
PNG
(CHEMBL4227537)
Show SMILES CCN(CC)c1cccc2nc3N(C(=O)CCn3c12)c1ccc(Cl)cc1Cl
Show InChI InChI=1S/C20H20Cl2N4O/c1-3-24(4-2)17-7-5-6-15-19(17)25-11-10-18(27)26(20(25)23-15)16-9-8-13(21)12-14(16)22/h5-9,12H,3-4,10-11H2,1-2H3
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Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method


Bioorg Med Chem 26: 2229-2250 (2018)


Article DOI: 10.1016/j.bmc.2018.01.020
BindingDB Entry DOI: 10.7270/Q2474DG1
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50234480
PNG
(CHEMBL4069551)
Show SMILES CCC(CC)c1ccc(Cl)c2nc(Oc3c(C)cc(Cl)cc3Cl)n(C)c12
Show InChI InChI=1S/C20H21Cl3N2O/c1-5-12(6-2)14-7-8-15(22)17-18(14)25(4)20(24-17)26-19-11(3)9-13(21)10-16(19)23/h7-10,12H,5-6H2,1-4H3
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Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Antagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of human CRF-stimulated cAMP accumulation


Bioorg Med Chem 25: 1556-1570 (2017)


Article DOI: 10.1016/j.bmc.2016.11.011
BindingDB Entry DOI: 10.7270/Q23R0W4P
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50460185
PNG
(CHEMBL4224781)
Show SMILES COc1nc(C)nc(OC)c1N1CCCn2c1nc1c(Cl)ccc(C(OC(F)F)C(F)(F)F)c21
Show InChI InChI=1S/C20H19ClF5N5O3/c1-9-27-16(32-2)14(17(28-9)33-3)31-8-4-7-30-13-10(15(20(24,25)26)34-18(22)23)5-6-11(21)12(13)29-19(30)31/h5-6,15,18H,4,7-8H2,1-3H3
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Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method


Bioorg Med Chem 26: 2229-2250 (2018)


Article DOI: 10.1016/j.bmc.2018.01.020
BindingDB Entry DOI: 10.7270/Q2474DG1
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50234473
PNG
(CHEMBL4091442)
Show SMILES CCN(CCO)c1ccc(Br)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12
Show InChI InChI=1S/C20H24BrClN4O2/c1-5-26(8-9-27)15-7-6-14(21)18-19(15)25(3)20(24-18)23-17-12(2)10-13(22)11-16(17)28-4/h6-7,10-11,27H,5,8-9H2,1-4H3,(H,23,24)
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Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition meas...


Bioorg Med Chem 25: 1556-1570 (2017)


Article DOI: 10.1016/j.bmc.2016.11.011
BindingDB Entry DOI: 10.7270/Q23R0W4P
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50460176
PNG
(CHEMBL4229125)
Show SMILES COc1ccc(N2CCCn3c2nc2c(Cl)ccc(C(OC(F)F)C(F)(F)F)c32)c(C)c1
Show InChI InChI=1S/C21H19ClF5N3O2/c1-11-10-12(31-2)4-7-15(11)29-8-3-9-30-17-13(18(21(25,26)27)32-19(23)24)5-6-14(22)16(17)28-20(29)30/h4-7,10,18-19H,3,8-9H2,1-2H3
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Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method


Bioorg Med Chem 26: 2229-2250 (2018)


Article DOI: 10.1016/j.bmc.2018.01.020
BindingDB Entry DOI: 10.7270/Q2474DG1
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50460182
PNG
(CHEMBL4225373)
Show SMILES COc1ccc(N2CCCn3c2nc2c(Cl)ccc(C(OC(F)F)C(F)(F)F)c32)c(C)n1
Show InChI InChI=1S/C20H18ClF5N4O2/c1-10-13(6-7-14(27-10)31-2)29-8-3-9-30-16-11(17(20(24,25)26)32-18(22)23)4-5-12(21)15(16)28-19(29)30/h4-7,17-18H,3,8-9H2,1-2H3
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Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method


Bioorg Med Chem 26: 2229-2250 (2018)


Article DOI: 10.1016/j.bmc.2018.01.020
BindingDB Entry DOI: 10.7270/Q2474DG1
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50536898
PNG
(CHEMBL4540030)
Show SMILES Cl.COCCN(c1ccc(Cl)cc1)c1cccc2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12
Show InChI InChI=1S/C25H26Cl2N4O2/c1-16-14-18(27)15-22(33-4)23(16)29-25-28-20-6-5-7-21(24(20)30(25)2)31(12-13-32-3)19-10-8-17(26)9-11-19/h5-11,14-15H,12-13H2,1-4H3,(H,28,29)
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Takeda Pharmaceutical Company Ltd

Curated by ChEMBL


Assay Description
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method


Bioorg Med Chem 24: 4675-4691 (2016)


Article DOI: 10.1016/j.bmc.2016.08.005
BindingDB Entry DOI: 10.7270/Q2G164BQ
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50460175
PNG
(CHEMBL4229070)
Show SMILES FC(F)OC(c1ccc(Cl)c2nc3N(CCCn3c12)c1ccc(Cl)cc1Cl)C(F)(F)F
Show InChI InChI=1S/C19H13Cl3F5N3O/c20-9-2-5-13(12(22)8-9)29-6-1-7-30-15-10(16(19(25,26)27)31-17(23)24)3-4-11(21)14(15)28-18(29)30/h2-5,8,16-17H,1,6-7H2
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Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method


Bioorg Med Chem 26: 2229-2250 (2018)


Article DOI: 10.1016/j.bmc.2018.01.020
BindingDB Entry DOI: 10.7270/Q2474DG1
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50536897
PNG
(CHEMBL4547748)
Show SMILES COc1cccc(c1)N(C(C)C)c1cccc2nc(Nc3c(C)cc(Br)cc3OC)n(C)c12
Show InChI InChI=1S/C26H29BrN4O2/c1-16(2)31(19-9-7-10-20(15-19)32-5)22-12-8-11-21-25(22)30(4)26(28-21)29-24-17(3)13-18(27)14-23(24)33-6/h7-16H,1-6H3,(H,28,29)
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Takeda Pharmaceutical Company Ltd

Curated by ChEMBL


Assay Description
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method


Bioorg Med Chem 24: 4675-4691 (2016)


Article DOI: 10.1016/j.bmc.2016.08.005
BindingDB Entry DOI: 10.7270/Q2G164BQ
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50234474
PNG
(CHEMBL4061900)
Show SMILES CCN(CC(C)O)c1ccc(Br)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12
Show InChI InChI=1S/C21H26BrClN4O2/c1-6-27(11-13(3)28)16-8-7-15(22)19-20(16)26(4)21(25-19)24-18-12(2)9-14(23)10-17(18)29-5/h7-10,13,28H,6,11H2,1-5H3,(H,24,25)
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Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition meas...


Bioorg Med Chem 25: 1556-1570 (2017)


Article DOI: 10.1016/j.bmc.2016.11.011
BindingDB Entry DOI: 10.7270/Q23R0W4P
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50536891
PNG
(CHEMBL4580457)
Show SMILES CNC(=O)c1cccc(c1)N(C(C)C)c1cccc2nc(Nc3c(C)cc(Br)cc3OC)n(C)c12
Show InChI InChI=1S/C27H30BrN5O2/c1-16(2)33(20-10-7-9-18(14-20)26(34)29-4)22-12-8-11-21-25(22)32(5)27(30-21)31-24-17(3)13-19(28)15-23(24)35-6/h7-16H,1-6H3,(H,29,34)(H,30,31)
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Takeda Pharmaceutical Company Ltd

Curated by ChEMBL


Assay Description
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method


Bioorg Med Chem 24: 4675-4691 (2016)


Article DOI: 10.1016/j.bmc.2016.08.005
BindingDB Entry DOI: 10.7270/Q2G164BQ
More data for this
Ligand-Target Pair
Corticotropin-releasing factor receptor 1


(Homo sapiens (Human))
BDBM50460168
PNG
(CHEMBL4225709)
Show SMILES COc1nc(C)c(N2CCCn3c2nc2c(Cl)ccc([C@@H](OC(F)F)C(F)(F)F)c32)c(C)n1 |r|
Show InChI InChI=1S/C20H19ClF5N5O2/c1-9-14(10(2)28-18(27-9)32-3)30-7-4-8-31-15-11(16(20(24,25)26)33-17(22)23)5-6-12(21)13(15)29-19(30)31/h5-6,16-17H,4,7-8H2,1-3H3/t16-/m1/s1
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Takeda Pharmaceutical Company Ltd.

Curated by ChEMBL


Assay Description
Antagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of human CRF-stimulated cAMP accumulation after 4 hrs by luc...


Bioorg Med Chem 26: 2229-2250 (2018)


Article DOI: 10.1016/j.bmc.2018.01.020
BindingDB Entry DOI: 10.7270/Q2474DG1
More data for this
Ligand-Target Pair
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