Reaction Details Report a problem with these data
Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM50241083
Substrate
n/a
Meas. Tech.
ChEMBL_1502758 (CHEMBL3591009)
Ki
0.340000±n/a nM
Citation
Devasthale, P; Wang, W; Hernandez, AS; Moore, F; Renduchintala, K; Sridhar, R; Pelleymounter, MA; Longhi, D; Huang, N; Flynn, N; Azzara, AV; Rohrbach, K; Devenny, J; Rooney, S; Thomas, M; Glick, S; Godonis, H; Harvey, S; Cullen, MJ; Zhang, H; Caporuscio, C; Stetsko, P; Grubb, M; Huang, C; Zhang, L; Freeden, C; Li, YX; Murphy, BJ; Robl, JA; Washburn, 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
More Info.:
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:
BDBM50241083
Synonyms:
6-(4-chlorophenyl)-3-(3-methoxy-4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)thieno[3,2-d]pyrimidin-4(3H)-one | CHEMBL214957 | GW-3430
Type:
Small organic molecule
Emp. Form.:
C25H24ClN3O3S
Mol. Mass.:
481.994
SMILES:
COc1cc(ccc1OCCN1CCCC1)-n1cnc2cc(sc2c1=O)-c1ccc(Cl)cc1