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Target
Gastrin/cholecystokinin type B receptor
Ligand
BDBM50348752
Substrate
n/a
Meas. Tech.
ChEMBL_757943 (CHEMBL1809360)
EC50
0.33±n/a nM
Citation
 Kolenc-Peitl, P; Mansi, R; Tamma, M; Gmeiner-Stopar, T; Sollner-Dolenc, M; Waser, B; Baum, RP; Reubi, JC; Maecke, HR Highly improved metabolic stability and pharmacokinetics of indium-111-DOTA-gastrin conjugates for targeting of the gastrin receptor. J Med Chem 54:2602-9 (2011) [PubMed]  Article 
Target
Name:
Gastrin/cholecystokinin type B receptor
Synonyms:
Cckbr | Cholecystokinin A | Cholecystokinin B receptor | Cholecystokinin receptor | GASR_RAT | Gastrin/cholecystokinin type B receptor
Type:
Enzyme Catalytic Domain
Mol. Mass.:
48980.43
Organism:
RAT
Description:
Cholecystokinin A CCKBR RAT::P30553
Residue:
452
Sequence:
MELLKLNRSVQGPGPGSGSSLCRPGVSLLNSSSAGNLSCDPPRIRGTGTRELEMAIRITLYAVIFLMSVGGNVLIIVVLGLSRRLRTVTNAFLLSLAVSDLLLAVACMPFTLLPNLMGTFIFGTVICKAISYLMGVSVSVSTLNLVAIALERYSAICRPLQARVWQTRSHAARVILATWLLSGLLMVPYPVYTMVQPVGPRVLQCMHRWPSARVQQTWSVLLLLLLFFIPGVVIAVAYGLISRELYLGLHFDGENDSETQSRARNQGGLPGGAAPGPVHQNGGCRPVTSVAGEDSDGCCVQLPRSRLEMTTLTTPTPGPVPGPRPNQAKLLAKKRVVRMLLVIVLLFFLCWLPVYSVNTWRAFDGPGAQRALSGAPISFIHLLSYVSACVNPLVYCFMHRRFRQACLDTCARCCPRPPRARPQPLPDEDPPTPSIASLSRLSYTTISTLGPG
  
Inhibitor
Name:
BDBM50348752
Synonyms:
CHEMBL1807150
Type:
Small organic molecule
Emp. Form.:
C71H103N13O23S
Mol. Mass.:
1538.716
SMILES:
CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](C)NCCOCCOCCOCCOCCOCCOC(=O)CN1CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC1)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O |r|
Structure:
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