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Compile Data Set for Download or QSAR

Found 464 hits Enz. Inhib. hit(s) with Target = 'Melanin-concentrating hormone receptor 1'   
Target
(Institution)
LigandTarget
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
Melanin-concentrating hormone receptor 1


(Mus musculus)
BDBM50383522
PNG
(CHEMBL2032049)
Show SMILES C[C@@H]1[C@H]2CN(CCC3(CCCCC3)C(O)=O)CC[C@@H]2Cc2[nH]c3ccc(cc3c12)C(F)(F)F
Show InChI InChI=1S/C26H33F3N2O2/c1-16-20-15-31(12-10-25(24(32)33)8-3-2-4-9-25)11-7-17(20)13-22-23(16)19-14-18(26(27,28)29)5-6-21(19)30-22/h5-6,14,16-17,20,30H,2-4,7-13,15H2,1H3,(H,32,33)/t16-,17-,20-/m1/s1
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n/an/a 0.600n/an/an/an/an/an/a



Amgen San Francisco

Curated by ChEMBL


Assay Description
Antagonist activity at mouse MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization


Bioorg Med Chem Lett 22: 3781-5 (2012)

More data for this
Ligand-Target Pair
Melanin-concentrating hormone receptor 1


(Macaca mulatta)
BDBM50383522
PNG
(CHEMBL2032049)
Show SMILES C[C@@H]1[C@H]2CN(CCC3(CCCCC3)C(O)=O)CC[C@@H]2Cc2[nH]c3ccc(cc3c12)C(F)(F)F
Show InChI InChI=1S/C26H33F3N2O2/c1-16-20-15-31(12-10-25(24(32)33)8-3-2-4-9-25)11-7-17(20)13-22-23(16)19-14-18(26(27,28)29)5-6-21(19)30-22/h5-6,14,16-17,20,30H,2-4,7-13,15H2,1H3,(H,32,33)/t16-,17-,20-/m1/s1
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n/an/a 0.800n/an/an/an/an/an/a



Amgen San Francisco

Curated by ChEMBL


Assay Description
Antagonist activity at rhesus monkey MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization


Bioorg Med Chem Lett 22: 3781-5 (2012)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50383522
PNG
(CHEMBL2032049)
Show SMILES C[C@@H]1[C@H]2CN(CCC3(CCCCC3)C(O)=O)CC[C@@H]2Cc2[nH]c3ccc(cc3c12)C(F)(F)F
Show InChI InChI=1S/C26H33F3N2O2/c1-16-20-15-31(12-10-25(24(32)33)8-3-2-4-9-25)11-7-17(20)13-22-23(16)19-14-18(26(27,28)29)5-6-21(19)30-22/h5-6,14,16-17,20,30H,2-4,7-13,15H2,1H3,(H,32,33)/t16-,17-,20-/m1/s1
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n/an/a 0.800n/an/an/an/an/an/a



Amgen San Francisco

Curated by ChEMBL


Assay Description
Antagonist activity at rat MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization


Bioorg Med Chem Lett 22: 3781-5 (2012)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50383112
PNG
(CHEMBL2029372)
Show SMILES Cc1c(NC(=O)c2ccc(cc2)-c2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12
Show InChI InChI=1S/C28H26FN3O/c1-19-26(13-10-24-16-20(17-30-27(19)24)18-32-14-2-3-15-32)31-28(33)23-6-4-21(5-7-23)22-8-11-25(29)12-9-22/h4-13,16-17H,2-3,14-15,18H2,1H3,(H,31,33)
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n/an/a 1n/an/an/an/an/an/a



Takeda Pharmaceutical Co., Ltd.

Curated by ChEMBL


Assay Description
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting


J Med Chem 55: 4336-51 (2012)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50388442
PNG
(CHEMBL2059408)
Show SMILES CCCCOc1ccc(cc1)C(=O)Nc1ccc2cc(CN3CCCC3)cnc2c1C
Show InChI InChI=1S/C26H31N3O2/c1-3-4-15-31-23-10-7-21(8-11-23)26(30)28-24-12-9-22-16-20(17-27-25(22)19(24)2)18-29-13-5-6-14-29/h7-12,16-17H,3-6,13-15,18H2,1-2H3,(H,28,30)
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n/an/a 1.20n/an/an/an/an/an/a



Takeda Pharmaceutical Co., Ltd.

Curated by ChEMBL


Assay Description
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting


J Med Chem 55: 4336-51 (2012)

More data for this
Ligand-Target Pair
Melanin-concentrating hormone receptor 1


(Mus musculus)
BDBM50162116
PNG
(2-(4-(benzyloxy)phenyl)-N-(1-(2-(pyrrolidin-1-yl)e...)
Show SMILES O=C(Cc1ccc(OCc2ccccc2)cc1)Nc1ccc2cnn(CCN3CCCC3)c2c1
Show InChI InChI=1S/C28H30N4O2/c33-28(18-22-8-12-26(13-9-22)34-21-23-6-2-1-3-7-23)30-25-11-10-24-20-29-32(27(24)19-25)17-16-31-14-4-5-15-31/h1-3,6-13,19-20H,4-5,14-18,21H2,(H,30,33)
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n/an/a 1.40n/an/an/an/an/an/a



Abbott Laboratories

Curated by ChEMBL


Assay Description
Inhibitory concentration against Melanin-concentrating hormone receptor 1 in diet-induced obese mice


Bioorg Med Chem Lett 15: 2752-7 (2005)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50388443
PNG
(CHEMBL2059409)
Show SMILES Cc1c(NC(=O)c2ccc(OCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12
Show InChI InChI=1S/C26H29N3O2/c1-18-24(28-26(30)21-6-9-23(10-7-21)31-17-19-4-5-19)11-8-22-14-20(15-27-25(18)22)16-29-12-2-3-13-29/h6-11,14-15,19H,2-5,12-13,16-17H2,1H3,(H,28,30)
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n/an/a 1.60n/an/an/an/an/an/a



Takeda Pharmaceutical Co., Ltd.

Curated by ChEMBL


Assay Description
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting


J Med Chem 55: 4336-51 (2012)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50383112
PNG
(CHEMBL2029372)
Show SMILES Cc1c(NC(=O)c2ccc(cc2)-c2ccc(F)cc2)ccc2cc(CN3CCCC3)cnc12
Show InChI InChI=1S/C28H26FN3O/c1-19-26(13-10-24-16-20(17-30-27(19)24)18-32-14-2-3-15-32)31-28(33)23-6-4-21(5-7-23)22-8-11-25(29)12-9-22/h4-13,16-17H,2-3,14-15,18H2,1H3,(H,31,33)
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n/an/a 1.70n/an/an/an/an/an/a



Takeda Pharmaceutical Company Limited

Curated by ChEMBL


Assay Description
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 1 hr by scintillation counting


J Med Chem 55: 2353-66 (2012)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50219047
PNG
(CHEMBL245231 | N-(3-(1-(4-(3,4-difluorophenoxy)ben...)
Show SMILES CC(C)C(=O)Nc1cccc(c1)C1CCN(Cc2ccc(Oc3ccc(F)c(F)c3)cc2)CC1
Show InChI InChI=1S/C28H30F2N2O2/c1-19(2)28(33)31-23-5-3-4-22(16-23)21-12-14-32(15-13-21)18-20-6-8-24(9-7-20)34-25-10-11-26(29)27(30)17-25/h3-11,16-17,19,21H,12-15,18H2,1-2H3,(H,31,33)
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n/an/a 1.80n/an/an/an/an/an/a



Tsukuba Research Institute

Curated by ChEMBL


Assay Description
Inhibition of rat MCH1R receptor


Bioorg Med Chem Lett 19: 5339-45 (2009)

More data for this
Ligand-Target Pair
Melanin-concentrating hormone receptor 1


(Mus musculus)
BDBM50167565
PNG
(1-[1-(2-Isobutylamino-ethyl)-1H-indazol-5-yl]-3-(4...)
Show SMILES CC(C)CNCCn1ncc2cc(NC(=O)Nc3ccc(Oc4ccccc4)cc3)ccc12
Show InChI InChI=1S/C26H29N5O2/c1-19(2)17-27-14-15-31-25-13-10-22(16-20(25)18-28-31)30-26(32)29-21-8-11-24(12-9-21)33-23-6-4-3-5-7-23/h3-13,16,18-19,27H,14-15,17H2,1-2H3,(H2,29,30,32)
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n/an/a 1.80n/an/an/an/an/an/a



Abbott Laboratories

Curated by ChEMBL


Assay Description
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]-MCH


Bioorg Med Chem Lett 15: 2752-7 (2005)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50388452
PNG
(CHEMBL2059420)
Show SMILES C[C@@H](N1CCCC1)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1
Show InChI InChI=1S/C27H31N3O2/c1-18-25(29-27(31)21-7-10-24(11-8-21)32-17-20-5-6-20)12-9-22-15-23(16-28-26(18)22)19(2)30-13-3-4-14-30/h7-12,15-16,19-20H,3-6,13-14,17H2,1-2H3,(H,29,31)/t19-/m1/s1
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n/an/a 1.90n/an/an/an/an/an/a



Takeda Pharmaceutical Co., Ltd.

Curated by ChEMBL


Assay Description
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting


J Med Chem 55: 4336-51 (2012)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50388444
PNG
(CHEMBL2059410)
Show SMILES Cc1c(NC(=O)c2ccc(OCCC3CC3)cc2)ccc2cc(CN3CCCC3)cnc12
Show InChI InChI=1S/C27H31N3O2/c1-19-25(11-8-23-16-21(17-28-26(19)23)18-30-13-2-3-14-30)29-27(31)22-6-9-24(10-7-22)32-15-12-20-4-5-20/h6-11,16-17,20H,2-5,12-15,18H2,1H3,(H,29,31)
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n/an/a 2n/an/an/an/an/an/a



Takeda Pharmaceutical Co., Ltd.

Curated by ChEMBL


Assay Description
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting


J Med Chem 55: 4336-51 (2012)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50351312
PNG
(CHEMBL1818800)
Show SMILES Clc1ccc(cc1)-c1ccc(cc1)C(=O)Nc1ccc2C=C(CN3CCCC3)CCc2c1
Show InChI InChI=1S/C28H27ClN2O/c29-26-12-9-22(10-13-26)21-5-7-23(8-6-21)28(32)30-27-14-11-24-17-20(3-4-25(24)18-27)19-31-15-1-2-16-31/h5-14,17-18H,1-4,15-16,19H2,(H,30,32)
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n/an/a 2.20n/an/an/an/an/an/a



Takeda Pharmaceutical Company Limited

Curated by ChEMBL


Assay Description
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting


Bioorg Med Chem 19: 5539-52 (2011)

More data for this
Ligand-Target Pair
Melanin-concentrating hormone receptor 1


(Mus musculus)
BDBM50167552
PNG
(1-[1-(2-Cyclopentylamino-ethyl)-1H-indazol-5-yl]-3...)
Show SMILES O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc2n(CCNC3CCCC3)ncc2c1
Show InChI InChI=1S/C27H29N5O2/c33-27(30-22-10-13-25(14-11-22)34-24-8-2-1-3-9-24)31-23-12-15-26-20(18-23)19-29-32(26)17-16-28-21-6-4-5-7-21/h1-3,8-15,18-19,21,28H,4-7,16-17H2,(H2,30,31,33)
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n/an/a 2.40n/an/an/an/an/an/a



Abbott Laboratories

Curated by ChEMBL


Assay Description
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]-MCH


Bioorg Med Chem Lett 15: 2752-7 (2005)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50388460
PNG
(CHEMBL2059513)
Show SMILES C[C@@H](NCCNC(C)=O)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1
Show InChI InChI=1S/C27H32N4O3/c1-17-25(31-27(33)21-6-9-24(10-7-21)34-16-20-4-5-20)11-8-22-14-23(15-30-26(17)22)18(2)28-12-13-29-19(3)32/h6-11,14-15,18,20,28H,4-5,12-13,16H2,1-3H3,(H,29,32)(H,31,33)/t18-/m1/s1
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n/an/a 2.40n/an/an/an/an/an/a



Takeda Pharmaceutical Co., Ltd.

Curated by ChEMBL


Assay Description
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting


J Med Chem 55: 4336-51 (2012)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50351322
PNG
(CHEMBL1818810)
Show SMILES Cc1ccc(cc1)-c1ccc(cc1)C(=O)Nc1ccc2C=C(CN3CCCC3)CCc2c1
Show InChI InChI=1S/C29H30N2O/c1-21-4-7-23(8-5-21)24-10-12-25(13-11-24)29(32)30-28-15-14-26-18-22(6-9-27(26)19-28)20-31-16-2-3-17-31/h4-5,7-8,10-15,18-19H,2-3,6,9,16-17,20H2,1H3,(H,30,32)
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n/an/a 2.40n/an/an/an/an/an/a



Takeda Pharmaceutical Company Limited

Curated by ChEMBL


Assay Description
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting


Bioorg Med Chem 19: 5539-52 (2011)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50351313
PNG
(CHEMBL1818801)
Show SMILES Clc1ccc(cc1)-c1ccc(cc1)C(=O)Nc1ccc2C=C(CN3CCCCC3)CCc2c1
Show InChI InChI=1S/C29H29ClN2O/c30-27-13-10-23(11-14-27)22-6-8-24(9-7-22)29(33)31-28-15-12-25-18-21(4-5-26(25)19-28)20-32-16-2-1-3-17-32/h6-15,18-19H,1-5,16-17,20H2,(H,31,33)
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n/an/a 2.5n/an/an/an/an/an/a



Takeda Pharmaceutical Company Limited

Curated by ChEMBL


Assay Description
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting


Bioorg Med Chem 19: 5539-52 (2011)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50388457
PNG
(CHEMBL2059426)
Show SMILES CC(NCC(C)(C)O)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1
Show InChI InChI=1S/C27H33N3O3/c1-17-24(30-26(31)20-7-10-23(11-8-20)33-15-19-5-6-19)12-9-21-13-22(14-28-25(17)21)18(2)29-16-27(3,4)32/h7-14,18-19,29,32H,5-6,15-16H2,1-4H3,(H,30,31)
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n/an/a 2.70n/an/an/an/an/an/a



Takeda Pharmaceutical Co., Ltd.

Curated by ChEMBL


Assay Description
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting


J Med Chem 55: 4336-51 (2012)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50351308
PNG
(CHEMBL1818795)
Show SMILES CN(C)CC1=Cc2ccc(NC(=O)c3ccc(cc3)-c3ccc(Cl)cc3)cc2CC1
Show InChI InChI=1S/C26H25ClN2O/c1-29(2)17-18-3-4-23-16-25(14-11-22(23)15-18)28-26(30)21-7-5-19(6-8-21)20-9-12-24(27)13-10-20/h5-16H,3-4,17H2,1-2H3,(H,28,30)
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n/an/a 2.70n/an/an/an/an/an/a



Takeda Pharmaceutical Company Limited

Curated by ChEMBL


Assay Description
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting


Bioorg Med Chem 19: 5539-52 (2011)

More data for this
Ligand-Target Pair
Melanin-concentrating hormone receptor 1


(Mus musculus)
BDBM50168509
PNG
(CHEMBL188937 | N-(1-Benzo[1,3]dioxol-5-ylmethyl-pi...)
Show SMILES COc1cc(cc(OC)c1C)C(=O)NC1CCCN(Cc2ccc3OCOc3c2)C1
Show InChI InChI=1S/C23H28N2O5/c1-15-20(27-2)10-17(11-21(15)28-3)23(26)24-18-5-4-8-25(13-18)12-16-6-7-19-22(9-16)30-14-29-19/h6-7,9-11,18H,4-5,8,12-14H2,1-3H3,(H,24,26)
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n/an/a 3n/an/an/an/an/an/a



Abbott Laboratories

Curated by ChEMBL


Assay Description
Inhibitory concentration required for binding affinity against mouse MCHr1 competing human neuronal IMR32 cells receptor in a radiometric binding ass...


Bioorg Med Chem Lett 15: 3412-6 (2005)

More data for this
Ligand-Target Pair
Melanin-concentrating hormone receptor 1


(Mus musculus)
BDBM119755
PNG
(US8685958, 4 | US8685958, 5)
Show SMILES COc1ccc(cc1)-c1nnc(o1)C(=O)N1CC(C1)Oc1ccc(CN2CC3(C2)CCCO3)cc1
Show InChI InChI=1S/C26H28N4O5/c1-32-20-9-5-19(6-10-20)23-27-28-24(35-23)25(31)30-14-22(15-30)34-21-7-3-18(4-8-21)13-29-16-26(17-29)11-2-12-33-26/h3-10,22H,2,11-17H2,1H3
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n/an/a 3n/an/an/an/an/an/a



AstraZeneca

Curated by ChEMBL


Assay Description
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis


J Med Chem 59: 2497-511 (2016)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50388458
PNG
(CHEMBL2059511)
Show SMILES CC(NCCNC(C)=O)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1
Show InChI InChI=1S/C27H32N4O3/c1-17-25(31-27(33)21-6-9-24(10-7-21)34-16-20-4-5-20)11-8-22-14-23(15-30-26(17)22)18(2)28-12-13-29-19(3)32/h6-11,14-15,18,20,28H,4-5,12-13,16H2,1-3H3,(H,29,32)(H,31,33)
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n/an/a 3.40n/an/an/an/an/an/a



Takeda Pharmaceutical Co., Ltd.

Curated by ChEMBL


Assay Description
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting


J Med Chem 55: 4336-51 (2012)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50351323
PNG
(CHEMBL1818811)
Show SMILES COc1ccc(cc1)-c1ccc(cc1)C(=O)Nc1ccc2C=C(CN3CCCC3)CCc2c1
Show InChI InChI=1S/C29H30N2O2/c1-33-28-14-11-23(12-15-28)22-6-8-24(9-7-22)29(32)30-27-13-10-25-18-21(4-5-26(25)19-27)20-31-16-2-3-17-31/h6-15,18-19H,2-5,16-17,20H2,1H3,(H,30,32)
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n/an/a 3.70n/an/an/an/an/an/a



Takeda Pharmaceutical Company Limited

Curated by ChEMBL


Assay Description
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting


Bioorg Med Chem 19: 5539-52 (2011)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50358743
PNG
(CHEMBL1922270)
Show SMILES C[C@@H]1[C@H]2CN(CCCC3CCOCC3)CC[C@@H]2Cc2[nH]c3ccc(cc3c12)C(F)(F)F
Show InChI InChI=1S/C25H33F3N2O/c1-16-21-15-30(9-2-3-17-7-11-31-12-8-17)10-6-18(21)13-23-24(16)20-14-19(25(26,27)28)4-5-22(20)29-23/h4-5,14,16-18,21,29H,2-3,6-13,15H2,1H3/t16-,18-,21-/m1/s1
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n/an/a 4n/an/an/an/an/an/a



Amgen

Curated by ChEMBL


Assay Description
Antagonist activity at rat MCHR1 expressed in HEK293 cells by aequorin bioluminescence assay


Bioorg Med Chem Lett 21: 7001-5 (2011)

More data for this
Ligand-Target Pair
Melanin-concentrating hormone receptor 1


(Macaca fascicularis)
BDBM50358743
PNG
(CHEMBL1922270)
Show SMILES C[C@@H]1[C@H]2CN(CCCC3CCOCC3)CC[C@@H]2Cc2[nH]c3ccc(cc3c12)C(F)(F)F
Show InChI InChI=1S/C25H33F3N2O/c1-16-21-15-30(9-2-3-17-7-11-31-12-8-17)10-6-18(21)13-23-24(16)20-14-19(25(26,27)28)4-5-22(20)29-23/h4-5,14,16-18,21,29H,2-3,6-13,15H2,1H3/t16-,18-,21-/m1/s1
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n/an/a 4n/an/an/an/an/an/a



Amgen

Curated by ChEMBL


Assay Description
Antagonist activity at cynomolgus monkey MCHR1


Bioorg Med Chem Lett 21: 7001-5 (2011)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50351324
PNG
(CHEMBL1818901)
Show SMILES Fc1ccc(cc1)-c1ccc(cc1)C(=O)Nc1ccc2C=C(CN3CCCC3)CCc2c1
Show InChI InChI=1S/C28H27FN2O/c29-26-12-9-22(10-13-26)21-5-7-23(8-6-21)28(32)30-27-14-11-24-17-20(3-4-25(24)18-27)19-31-15-1-2-16-31/h5-14,17-18H,1-4,15-16,19H2,(H,30,32)
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n/an/a 4.10n/an/an/an/an/an/a



Takeda Pharmaceutical Company Limited

Curated by ChEMBL


Assay Description
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting


Bioorg Med Chem 19: 5539-52 (2011)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50388450
PNG
(CHEMBL2059418)
Show SMILES CC(N1CCCC1)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1
Show InChI InChI=1S/C27H31N3O2/c1-18-25(29-27(31)21-7-10-24(11-8-21)32-17-20-5-6-20)12-9-22-15-23(16-28-26(18)22)19(2)30-13-3-4-14-30/h7-12,15-16,19-20H,3-6,13-14,17H2,1-2H3,(H,29,31)
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n/an/a 4.20n/an/an/an/an/an/a



Takeda Pharmaceutical Co., Ltd.

Curated by ChEMBL


Assay Description
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting


J Med Chem 55: 4336-51 (2012)

More data for this
Ligand-Target Pair
Melanin-concentrating hormone receptor 1


(Mus musculus)
BDBM50192518
PNG
(1-(2-(3,4-dimethylphenoxy)-5-((2-(pyrrolidin-1-yl)...)
Show SMILES Cc1ccc(Oc2ccc(cc2NC(=O)Nc2ccccc2)C(=O)NCCN2CCCC2)cc1C
Show InChI InChI=1S/C28H32N4O3/c1-20-10-12-24(18-21(20)2)35-26-13-11-22(27(33)29-14-17-32-15-6-7-16-32)19-25(26)31-28(34)30-23-8-4-3-5-9-23/h3-5,8-13,18-19H,6-7,14-17H2,1-2H3,(H,29,33)(H2,30,31,34)
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n/an/a 5n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA


Bioorg Med Chem Lett 16: 5066-72 (2006)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50351314
PNG
(CHEMBL1818802)
Show SMILES CN1CCN(CC2=Cc3ccc(NC(=O)c4ccc(cc4)-c4ccc(Cl)cc4)cc3CC2)CC1
Show InChI InChI=1S/C29H30ClN3O/c1-32-14-16-33(17-15-32)20-21-2-3-26-19-28(13-10-25(26)18-21)31-29(34)24-6-4-22(5-7-24)23-8-11-27(30)12-9-23/h4-13,18-19H,2-3,14-17,20H2,1H3,(H,31,34)
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n/an/a 5.30n/an/an/an/an/an/a



Takeda Pharmaceutical Company Limited

Curated by ChEMBL


Assay Description
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting


Bioorg Med Chem 19: 5539-52 (2011)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50351297
PNG
(CHEMBL1818783)
Show SMILES CN(C)CC1CCc2cc(NC(=O)c3ccc(cc3)-c3ccc(Cl)cc3)ccc2C1
Show InChI InChI=1S/C26H27ClN2O/c1-29(2)17-18-3-4-23-16-25(14-11-22(23)15-18)28-26(30)21-7-5-19(6-8-21)20-9-12-24(27)13-10-20/h5-14,16,18H,3-4,15,17H2,1-2H3,(H,28,30)
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n/an/a 5.30n/an/an/an/an/an/a



Takeda Pharmaceutical Company Limited

Curated by ChEMBL


Assay Description
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting


Bioorg Med Chem 19: 5539-52 (2011)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50388454
PNG
(CHEMBL2059422)
Show SMILES CC(N1CCCCCC1)c1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1
Show InChI InChI=1S/C29H35N3O2/c1-20-27(31-29(33)23-9-12-26(13-10-23)34-19-22-7-8-22)14-11-24-17-25(18-30-28(20)24)21(2)32-15-5-3-4-6-16-32/h9-14,17-18,21-22H,3-8,15-16,19H2,1-2H3,(H,31,33)
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n/an/a 5.60n/an/an/an/an/an/a



Takeda Pharmaceutical Co., Ltd.

Curated by ChEMBL


Assay Description
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting


J Med Chem 55: 4336-51 (2012)

More data for this
Ligand-Target Pair
Melanin-concentrating hormone receptor 1


(Mus musculus)
BDBM50167554
PNG
(1-(4-Phenoxy-phenyl)-3-[1-(2-pyrrolidin-1-yl-ethyl...)
Show SMILES O=c1n(ccn1-c1ccc2n(CCN3CCCC3)ncc2c1)-c1ccc(Oc2ccccc2)cc1
Show InChI InChI=1S/C28H27N5O2/c34-28-31(23-8-11-26(12-9-23)35-25-6-2-1-3-7-25)17-18-32(28)24-10-13-27-22(20-24)21-29-33(27)19-16-30-14-4-5-15-30/h1-3,6-13,17-18,20-21H,4-5,14-16,19H2
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n/an/a 5.90n/an/an/an/an/an/a



Abbott Laboratories

Curated by ChEMBL


Assay Description
Inhibitory concentration against mouse Melanin-concentrating hormone receptor 1 expressed in IMR-32 cells using [125I]-MCH


Bioorg Med Chem Lett 15: 2752-7 (2005)

More data for this
Ligand-Target Pair
Melanin-concentrating hormone receptor 1


(Mus musculus)
BDBM50159340
PNG
(CHEMBL3786169)
Show SMILES COc1ccc(cc1)-c1nnc(o1)C(=O)N1CC(C1)Oc1ccc(CN2CCCC2)cc1
Show InChI InChI=1S/C24H26N4O4/c1-30-19-10-6-18(7-11-19)22-25-26-23(32-22)24(29)28-15-21(16-28)31-20-8-4-17(5-9-20)14-27-12-2-3-13-27/h4-11,21H,2-3,12-16H2,1H3
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n/an/a 6n/an/an/an/an/an/a



AstraZeneca

Curated by ChEMBL


Assay Description
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis


J Med Chem 59: 2497-511 (2016)

More data for this
Ligand-Target Pair
Melanin-concentrating hormone receptor 1


(Mus musculus)
BDBM50159145
PNG
(CHEMBL3786685)
Show SMILES CC1(O)CCN(Cc2ccc(OC3CN(C3)C(=O)c3nnc(o3)-c3ccccc3)cc2)C1
Show InChI InChI=1/C24H26N4O4/c1-24(30)11-12-27(16-24)13-17-7-9-19(10-8-17)31-20-14-28(15-20)23(29)22-26-25-21(32-22)18-5-3-2-4-6-18/h2-10,20,30H,11-16H2,1H3
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n/an/a 6n/an/an/an/an/an/a



AstraZeneca

Curated by ChEMBL


Assay Description
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis


J Med Chem 59: 2497-511 (2016)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50391543
PNG
(CHEMBL2147477)
Show SMILES C[C@@H](CNCc1ccccc1)N1C[C@H](CCCN=C(N)N)N(CCc2cccc(F)c2)C1=S
Show InChI InChI=1S/C25H35FN6S/c1-19(16-29-17-21-7-3-2-4-8-21)32-18-23(11-6-13-30-24(27)28)31(25(32)33)14-12-20-9-5-10-22(26)15-20/h2-5,7-10,15,19,23,29H,6,11-14,16-18H2,1H3,(H4,27,28,30)/t19-,23-/m0/s1
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n/an/a 6.10n/an/an/an/an/an/a



LEO Pharma

Curated by ChEMBL


Assay Description
Antagonist activity at rat MCH1 receptor expressed in HEK 293T cells assessed as inhibition of MCH-induced Ca2+ mobilization after 10 mins by FLIPR a...


Bioorg Med Chem Lett 22: 6039-47 (2012)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50351318
PNG
(CHEMBL1818806)
Show SMILES CCC(=O)N(C)CC1=Cc2ccc(NC(=O)c3ccc(cc3)-c3ccc(Cl)cc3)cc2CC1
Show InChI InChI=1S/C28H27ClN2O2/c1-3-27(32)31(2)18-19-4-5-24-17-26(15-12-23(24)16-19)30-28(33)22-8-6-20(7-9-22)21-10-13-25(29)14-11-21/h6-17H,3-5,18H2,1-2H3,(H,30,33)
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n/an/a 6.20n/an/an/an/an/an/a



Takeda Pharmaceutical Company Limited

Curated by ChEMBL


Assay Description
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting


Bioorg Med Chem 19: 5539-52 (2011)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50351297
PNG
(CHEMBL1818783)
Show SMILES CN(C)CC1CCc2cc(NC(=O)c3ccc(cc3)-c3ccc(Cl)cc3)ccc2C1
Show InChI InChI=1S/C26H27ClN2O/c1-29(2)17-18-3-4-23-16-25(14-11-22(23)15-18)28-26(30)21-7-5-19(6-8-21)20-9-12-24(27)13-10-20/h5-14,16,18H,3-4,15,17H2,1-2H3,(H,28,30)
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n/an/a 6.20n/an/an/an/an/an/a



Takeda Pharmaceutical Company Limited

Curated by ChEMBL


Assay Description
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting


Bioorg Med Chem 19: 5539-52 (2011)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50149456
PNG
(CHEMBL3769702)
Show SMILES Cc1c(nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cn12)C1CC1
Show InChI InChI=1S/C20H18F3N3O3/c1-12-19(13-2-3-13)25-17-9-4-14(10-26(12)17)24-18(27)11-28-15-5-7-16(8-6-15)29-20(21,22)23/h4-10,13H,2-3,11H2,1H3,(H,24,27)
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n/an/a 6.30n/an/an/an/an/an/a



Takeda Pharmaceutical Co., Ltd.

Curated by ChEMBL


Assay Description
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis


J Med Chem 59: 1116-39 (2016)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50357508
PNG
(CHEMBL1914637)
Show SMILES CCS(=O)(=O)N1CCc2ccc(cc2CC1)C(=O)CCCN1CCC(CC1)c1ccc(Cl)cc1
Show InChI InChI=1S/C27H35ClN2O3S/c1-2-34(32,33)30-18-13-22-5-6-25(20-24(22)14-19-30)27(31)4-3-15-29-16-11-23(12-17-29)21-7-9-26(28)10-8-21/h5-10,20,23H,2-4,11-19H2,1H3
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n/an/a 6.40n/an/an/an/an/an/a



Takeda Pharmaceutical Co., Ltd

Curated by ChEMBL


Assay Description
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells


Bioorg Med Chem 19: 6261-73 (2011)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50388449
PNG
(CHEMBL2059417)
Show SMILES CC1CCCN1Cc1cnc2c(C)c(NC(=O)c3ccc(OCC4CC4)cc3)ccc2c1
Show InChI InChI=1S/C27H31N3O2/c1-18-4-3-13-30(18)16-21-14-23-9-12-25(19(2)26(23)28-15-21)29-27(31)22-7-10-24(11-8-22)32-17-20-5-6-20/h7-12,14-15,18,20H,3-6,13,16-17H2,1-2H3,(H,29,31)
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n/an/a 6.70n/an/an/an/an/an/a



Takeda Pharmaceutical Co., Ltd.

Curated by ChEMBL


Assay Description
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting


J Med Chem 55: 4336-51 (2012)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50388445
PNG
(CHEMBL2059411)
Show SMILES CC(C)COc1ccc(cc1)C(=O)Nc1ccc2cc(CN3CCCC3)cnc2c1C
Show InChI InChI=1S/C26H31N3O2/c1-18(2)17-31-23-9-6-21(7-10-23)26(30)28-24-11-8-22-14-20(15-27-25(22)19(24)3)16-29-12-4-5-13-29/h6-11,14-15,18H,4-5,12-13,16-17H2,1-3H3,(H,28,30)
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n/an/a 6.70n/an/an/an/an/an/a



Takeda Pharmaceutical Co., Ltd.

Curated by ChEMBL


Assay Description
Displacement of [125I]MCH from rat MCHR1 expressed in CHO cells after 60 mins by liquid scintillation counting


J Med Chem 55: 4336-51 (2012)

More data for this
Ligand-Target Pair
Melanin-concentrating hormone receptor 1


(Mus musculus)
BDBM50159339
PNG
(CHEMBL3786841)
Show SMILES COc1ccc(cc1)-c1nnc(o1)C(=O)N1CC(C1)Oc1ccc(CN2CC3(C2)CCOC3)cc1
Show InChI InChI=1S/C26H28N4O5/c1-32-20-8-4-19(5-9-20)23-27-28-24(35-23)25(31)30-13-22(14-30)34-21-6-2-18(3-7-21)12-29-15-26(16-29)10-11-33-17-26/h2-9,22H,10-17H2,1H3
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n/an/a 7n/an/an/an/an/an/a



AstraZeneca

Curated by ChEMBL


Assay Description
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis


J Med Chem 59: 2497-511 (2016)

More data for this
Ligand-Target Pair
Melanin-concentrating hormone receptor 1


(Mus musculus)
BDBM50159341
PNG
(CHEMBL3786346)
Show SMILES O=C(N1CC(C1)Oc1ccc(CN2CC3(C2)CCCO3)cc1)c1nnc(o1)-c1ccccc1
Show InChI InChI=1S/C25H26N4O4/c30-24(23-27-26-22(33-23)19-5-2-1-3-6-19)29-14-21(15-29)32-20-9-7-18(8-10-20)13-28-16-25(17-28)11-4-12-31-25/h1-3,5-10,21H,4,11-17H2
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n/an/a 7n/an/an/an/an/an/a



AstraZeneca

Curated by ChEMBL


Assay Description
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis


J Med Chem 59: 2497-511 (2016)

More data for this
Ligand-Target Pair
Melanin-concentrating hormone receptor 1


(Mus musculus)
BDBM119758
PNG
(US8685958, 7 | US8685958, 8)
Show SMILES O=C(N1CC(C1)Oc1ccc(CN2CC3(C2)CCOC3)cc1)c1nnc(o1)-c1ccccc1
Show InChI InChI=1S/C25H26N4O4/c30-24(23-27-26-22(33-23)19-4-2-1-3-5-19)29-13-21(14-29)32-20-8-6-18(7-9-20)12-28-15-25(16-28)10-11-31-17-25/h1-9,21H,10-17H2
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n/an/a 7n/an/an/an/an/an/a



AstraZeneca

Curated by ChEMBL


Assay Description
Displacement of [125I]Tyr13-MCH from mouse MCHR1 after 60 mins by microbeta scintillation counting analysis


J Med Chem 59: 2497-511 (2016)

More data for this
Ligand-Target Pair
Melanin-concentrating hormone receptor 1


(Mus musculus)
BDBM50192531
PNG
(1-(2-chlorophenyl)-3-(2-(3,4-dimethylphenoxy)-5-((...)
Show SMILES Cc1ccc(Oc2ccc(cc2NC(=O)Nc2ccccc2Cl)C(=O)NCCN2CCCC2)cc1C
Show InChI InChI=1S/C28H31ClN4O3/c1-19-9-11-22(17-20(19)2)36-26-12-10-21(27(34)30-13-16-33-14-5-6-15-33)18-25(26)32-28(35)31-24-8-4-3-7-23(24)29/h3-4,7-12,17-18H,5-6,13-16H2,1-2H3,(H,30,34)(H2,31,32,35)
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n/an/a 7n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of [125I]MCH binding to mouse MCHR1 expressed in HEK293 cells by HT-SPA


Bioorg Med Chem Lett 16: 5066-72 (2006)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50357504
PNG
(CHEMBL1914633)
Show SMILES Clc1ccc(cc1)C1CCN(CCCC(=O)c2ccc3CCN(CCc3c2)C(=O)C2CC2)CC1
Show InChI InChI=1S/C29H35ClN2O2/c30-27-9-7-21(8-10-27)23-11-16-31(17-12-23)15-1-2-28(33)26-6-3-22-13-18-32(19-14-25(22)20-26)29(34)24-4-5-24/h3,6-10,20,23-24H,1-2,4-5,11-19H2
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n/an/a 7.30n/an/an/an/an/an/a



Takeda Pharmaceutical Co., Ltd

Curated by ChEMBL


Assay Description
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells


Bioorg Med Chem 19: 6261-73 (2011)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50149462
PNG
(CHEMBL3771182)
Show SMILES Cc1c(nc2ccc(cn12)-n1ccc(OCc2csc(Cl)c2)cc1=O)C1CC1
Show InChI InChI=1S/C21H18ClN3O2S/c1-13-21(15-2-3-15)23-19-5-4-16(10-25(13)19)24-7-6-17(9-20(24)26)27-11-14-8-18(22)28-12-14/h4-10,12,15H,2-3,11H2,1H3
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n/an/a 7.5n/an/an/an/an/an/a



Takeda Pharmaceutical Co., Ltd.

Curated by ChEMBL


Assay Description
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis


J Med Chem 59: 1116-39 (2016)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50357503
PNG
(CHEMBL1914632)
Show SMILES CCCC(=O)N1CCc2ccc(cc2CC1)C(=O)CCCN1CCC(CC1)c1ccc(Cl)cc1
Show InChI InChI=1S/C29H37ClN2O2/c1-2-4-29(34)32-19-14-23-6-7-26(21-25(23)15-20-32)28(33)5-3-16-31-17-12-24(13-18-31)22-8-10-27(30)11-9-22/h6-11,21,24H,2-5,12-20H2,1H3
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n/an/a 7.5n/an/an/an/an/an/a



Takeda Pharmaceutical Co., Ltd

Curated by ChEMBL


Assay Description
Displacement of [125I]-MCH(4-19) from rat MCHR1 expressed in CHO cells


Bioorg Med Chem 19: 6261-73 (2011)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50189576
PNG
((R)-6-(6-(3-(methylamino)pyrrolidin-1-yl)pyridin-3...)
Show SMILES CN[C@@H]1CCN(C1)c1ccc(cn1)-n1ncc2cc(sc2c1=O)-c1ccc(cc1)C(F)(F)F
Show InChI InChI=1S/C23H20F3N5OS/c1-27-17-8-9-30(13-17)20-7-6-18(12-28-20)31-22(32)21-15(11-29-31)10-19(33-21)14-2-4-16(5-3-14)23(24,25)26/h2-7,10-12,17,27H,8-9,13H2,1H3/t17-/m1/s1
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n/an/a 7.70n/an/an/an/an/an/a



Neurocrine Biosciences Inc.

Curated by ChEMBL


Assay Description
Activity at chimeric rat/human MCH1R by accumulation of GTPgammaS


J Med Chem 49: 3753-6 (2006)

More data for this
Ligand-Target Pair
GPR24


(RAT)
BDBM50149457
PNG
(CHEMBL3771335)
Show SMILES Cc1nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cn2c1C
Show InChI InChI=1S/C18H16F3N3O3/c1-11-12(2)24-9-13(3-8-16(24)22-11)23-17(25)10-26-14-4-6-15(7-5-14)27-18(19,20)21/h3-9H,10H2,1-2H3,(H,23,25)
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n/an/a 7.80n/an/an/an/an/an/a



Takeda Pharmaceutical Co., Ltd.

Curated by ChEMBL


Assay Description
Displacement of [125I]-MCH (4 to 19 residues) from rat MCHR1 expressed in CHO cell membranes after 1 hr by liquid scintillation counting analysis


J Med Chem 59: 1116-39 (2016)

More data for this
Ligand-Target Pair
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