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Target
Gastrin/cholecystokinin type B receptor
Ligand
BDBM50318666
Substrate
n/a
Meas. Tech.
ChEMBL_658540 (CHEMBL1247742)
IC50
>30000±n/a nM
Citation
Rottmann, M; McNamara, C; Yeung, BK; Lee, MC; Zou, B; Russell, B; Seitz, P; Plouffe, DM; Dharia, NV; Tan, J; Cohen, SB; Spencer, KR; González-Páez, GE; Lakshminarayana, SB; Goh, A; Suwanarusk, R; Jegla, T; Schmitt, EK; Beck, HP; Brun, R; Nosten, F; Renia, L; Dartois, V; Keller, TH; Fidock, DA; Winzeler, EA; Diagana, TT Spiroindolones, a potent compound class for the treatment of malaria. Science 329:1175-80 (2010) [PubMed] Article
More Info.:
Target
Name:
Gastrin/cholecystokinin type B receptor
Synonyms:
CCK-2 receptor | CCK-B receptor | CCK-BR | CCKBR | CCKRB | Cholecystokinin A | Cholecystokinin receptor | Cholecystokinin-2 Receptor | GASR_HUMAN | Gastrin/cholecystokinin type B receptor
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
48445.79
Organism:
Homo sapiens (Human)
Description:
Stable expression of human CCK-2 receptors in HEK 293 cells.
Residue:
447
Sequence:
MELLKLNRSVQGTGPGPGASLCRPGAPLLNSSSVGNLSCEPPRIRGAGTRELELAIRITLYAVIFLMSVGGNMLIIVVLGLSRRLRTVTNAFLLSLAVSDLLLAVACMPFTLLPNLMGTFIFGTVICKAVSYLMGVSVSVSTLSLVAIALERYSAICRPLQARVWQTRSHAARVIVATWLLSGLLMVPYPVYTVVQPVGPRVLQCVHRWPSARVRQTWSVLLLLLLFFIPGVVMAVAYGLISRELYLGLRFDGDSDSDSQSRVRNQGGLPGAVHQNGRCRPETGAVGEDSDGCYVQLPRSRPALELTALTAPGPGSGSRPTQAKLLAKKRVVRMLLVIVVLFFLCWLPVYSANTWRAFDGPGAHRALSGAPISFIHLLSYASACVNPLVYCFMHRRFRQACLETCARCCPRPPRARPRALPDEDPPTPSIASLSRLSYTTISTLGPG
Inhibitor
Name:
BDBM50318666
Synonyms:
(1R,3S)-5',7-Dichloro-6-fluoro-3-methyl-2,3,4,9-tetrahydrospiro-[beta-carboline-1,3'-indol]-2'(1'H)-one | CHEMBL1082723 | NITD609
Type:
Small organic molecule
Emp. Form.:
C19H14Cl2FN3O
Mol. Mass.:
390.238
SMILES:
C[C@H]1Cc2c([nH]c3cc(Cl)c(F)cc23)[C@@]2(N1)C(=O)Nc1ccc(Cl)cc21 |r|