Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM50241083
Substrate
n/a
Meas. Tech.
ChEMBL_1502758 (CHEMBL3591009)
Ki
0.340000±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:
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
Structure:
Search PDB for entries with ligand similarity: