Target
Cholecystokinin receptor type A
Ligand
BDBM50061829
Substrate
n/a
Meas. Tech.
ChEMBL_1868964 (CHEMBL4370030)
IC50
0.044668±n/a nM
Citation
 Sensfuss, UKruse, TSkyggebjerg, RBUldam, HKVestergaard, BHuus, KVinther, TNReinau, MESchéele, SClausen, TR Structure-Activity Relationships and Characterization of Highly Selective, Long-Acting, Peptide-Based Cholecystokinin 1 Receptor Agonists. J Med Chem 62:1407-1419 (2019) [PubMed]  Article 
Target
Name:
Cholecystokinin receptor type A
Synonyms:
CCK-A receptor | CCK-AR | CCK1-R | CCKAR | CCKAR_HUMAN | CCKRA | Cholecystokinin receptor | Cholecystokinin receptor type A | Cholecystokinin-1 Receptor
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
47859.34
Organism:
Homo sapiens (Human)
Description:
Stable expression of human CCK-1 receptors in HEK 293 cells.
Residue:
428
Sequence:
MDVVDSLLVNGSNITPPCELGLENETLFCLDQPRPSKEWQPAVQILLYSLIFLLSVLGNTLVITVLIRNKRMRTVTNIFLLSLAVSDLMLCLFCMPFNLIPNLLKDFIFGSAVCKTTTYFMGTSVSVSTFNLVAISLERYGAICKPLQSRVWQTKSHALKVIAATWCLSFTIMTPYPIYSNLVPFTKNNNQTANMCRFLLPNDVMQQSWHTFLLLILFLIPGIVMMVAYGLISLELYQGIKFEASQKKSAKERKPSTTSSGKYEDSDGCYLQKTRPPRKLELRQLSTGSSSRANRIRSNSSAANLMAKKRVIRMLIVIVVLFFLCWMPIFSANAWRAYDTASAERRLSGTPISFILLLSYTSSCVNPIIYCFMNKRFRLGFMATFPCCPNPGPPGARGEVGEEEEGGTTGASLSRFSYSHMSASVPPQ
  
Inhibitor
Name:
BDBM50061829
Synonyms:
(R)-N-((S)-1-Carbamoyl-2-phenyl-ethyl)-3-({(S)-2-[(S)-3-(1H-indol-3-yl)-2-(2-{(S)-2-[2-(4-sulfooxy-phenyl)-acetylamino]-hexanoylamino}-acetylamino)-propionylamino]-hexanoyl}-methyl-amino)-succinamic acid | CHEMBL423907
Type:
Small organic molecule
Emp. Form.:
C47H60N8O13S
Mol. Mass.:
977.09
SMILES:
CCCC[C@H](NC(=O)Cc1ccc(OS(O)(=O)=O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N(C)[C@H](CC(O)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O
Structure:
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