Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM50094885
Substrate
n/a
Meas. Tech.
ChEMBL_1502790 (CHEMBL3591193)
Ki
3.8±n/a nM
Citation
 Devasthale, PWang, WHernandez, ASMoore, FRenduchintala, KSridhar, RPelleymounter, MALonghi, DHuang, NFlynn, NAzzara, AVRohrbach, KDevenny, JRooney, SThomas, MGlick, SGodonis, HHarvey, SCullen, MJZhang, HCaporuscio, CStetsko, PGrubb, MHuang, CZhang, LFreeden, CLi, YXMurphy, BJRobl, JAWashburn, WN Dihydropyrrolopyrazol-6-one MCHR1 antagonists for the treatment of obesity: Insights on in vivo efficacy from a novel FLIPR assay setup. Bioorg Med Chem Lett 25:2793-9 (2015) [PubMed]  Article 
Target
Name:
Melanin-concentrating hormone receptor 1
Synonyms:
G-protein coupled receptor 24 | Gpr24 | MCH receptor 1 | MCH-1R | MCH-R1 | MCH1R | MCHR | MCHR-1 | MCHR1_RAT | Mchr1 | Melanin Concentrating Hormone 1 | Melanin-concentrating hormone receptor | Melanin-concentrating hormone receptor 1 | SLC-1 | Slc1 | Somatostatin receptor-like protein
Type:
Enzyme Catalytic Domain
Mol. Mass.:
39075.64
Organism:
RAT
Description:
Melanin Concentrating Hormone 1 GPR24 RAT::P97639
Residue:
353
Sequence:
MDLQTSLLSTGPNASNISDGQDNLTLPGSPPRTGSVSYINIIMPSVFGTICLLGIVGNSTVIFAVVKKSKLHWCSNVPDIFIINLSVVDLLFLLGMPFMIHQLMGNGVWHFGETMCTLITAMDANSQFTSTYILTAMTIDRYLATVHPISSTKFRKPSMATLVICLLWALSFISITPVWLYARLIPFPGGAVGCGIRLPNPDTDLYWFTLYQFFLAFALPFVVITAAYVKILQRMTSSVAPASQRSIRLRTKRVTRTAIAICLVFFVCWAPYYVLQLTQLSISRPTLTFVYLYNAAISLGYANSCLNPFVYIVLCETFRKRLVLSVKPAAQGQLRTVSNAQTADEERTESKGT
  
Inhibitor
Name:
BDBM50094885
Synonyms:
CHEMBL3588863
Type:
Small organic molecule
Emp. Form.:
C24H25ClN4O5
Mol. Mass.:
484.932
SMILES:
COc1cc(ccc1OCC(C)(C)OC(=O)CN)N1Cc2cn(nc2C1=O)-c1ccc(Cl)cc1
Structure:
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