Reaction Details Report a problem with these data
Target
Gastrin/cholecystokinin type B receptor
Ligand
BDBM50024321
Substrate
n/a
Meas. Tech.
ChEMBL_2024091 (CHEMBL4677904)
EC50
2.8±n/a nM
Citation
Klingler, M; Hörmann, AA; Rangger, C; Desrues, L; Castel, H; Gandolfo, P; von Guggenberg, E Stabilization Strategies for Linear Minigastrin Analogues: Further Improvements J Med Chem 63:14668-14679 (2020) [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:
BDBM50024321
Synonyms:
3-{2-[2-(3-tert-Butoxycarbonylamino-propionylamino)-3-(1H-indol-3-yl)-propionylamino]-4-methylsulfanyl-butyrylamino}-N-(1-carbamoyl-2-phenyl-ethyl)-succinamic acid | AY-6608 | CHEMBL1328 | ICI-50123 | PENTAGASTRIN | Peptavlon
Type:
Small organic molecule
Emp. Form.:
C37H49N7O9S
Mol. Mass.:
767.891
SMILES:
CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCNC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O