Reaction Details Report a problem with these data
Target
Gastrin-releasing peptide receptor
Ligand
BDBM50071739
Substrate
n/a
Meas. Tech.
ChEMBL_39762 (CHEMBL883283)
IC50
16±n/a nM
Citation
Ashwood, V; Brownhill, V; Higginbottom, M; Horwell, DC; Hughes, J; Lewthwaite, RA; McKnight, AT; Pinnock, RD; Pritchard, MC; Suman-Chauhan, N; Webb, C; Williams, SC PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist. Bioorg Med Chem Lett 8:2589-94 (1999) [PubMed] Article
More Info.:
Target
Name:
Gastrin-releasing peptide receptor
Synonyms:
Bombesin 2 | GRP-R | GRP-preferring bombesin receptor | GRPR | GRPR_HUMAN | Gastrin releasing peptide receptor | Gastrin-releasing peptide receptor
Type:
Enzyme Catalytic Domain
Mol. Mass.:
43214.53
Organism:
Homo sapiens (Human)
Description:
Bombesin 2 GRPR 0::P30550
Residue:
384
Sequence:
MALNDCFLLNLEVDHFMHCNISSHSADLPVNDDWSHPGILYVIPAVYGVIILIGLIGNITLIKIFCTVKSMRNVPNLFISSLALGDLLLLITCAPVDASRYLADRWLFGRIGCKLIPFIQLTSVGVSVFTLTALSADRYKAIVRPMDIQASHALMKICLKAAFIWIISMLLAIPEAVFSDLHPFHEESTNQTFISCAPYPHSNELHPKIHSMASFLVFYVIPLSIISVYYYFIAKNLIQSAYNLPVEGNIHVKKQIESRKRLAKTVLVFVGLFAFCWLPNHVIYLYRSYHYSEVDTSMLHFVTSICARLLAFTNSCVNPFALYLLSKSFRKQFNTQLLCCQPGLIIRSHSTGRSTTCMTSLKSTNPSVATFSLINGNICHERYV
Inhibitor
Name:
BDBM50071739
Synonyms:
(S)-3-(1H-Indol-3-yl)-N-[1-(5-methoxy-pyridin-2-yl)-cyclohexylmethyl]-2-methyl-2-[3-(4-nitro-phenyl)-ureido]-propionamide | CHEMBL405908
Type:
Small organic molecule
Emp. Form.:
C32H36N6O5
Mol. Mass.:
584.6654
SMILES:
COc1ccc(nc1)C1(CNC(=O)[C@](C)(Cc2c[nH]c3ccccc23)NC(=O)Nc2ccc(cc2)[N+]([O-])=O)CCCCC1