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Target
Gastric inhibitory polypeptide receptor
Ligand
BDBM29130
Substrate
125I-GIP
Meas. Tech.
SPA Receptor Binding Assay
IC50
381±n/a nM
Citation
 Madsen, P; Kodra, JT; Behrens, C; Nishimura, E; Jeppesen, CB; Pridal, L; Andersen, B; Knudsen, LB; Valcarce-Aspegren, C; Guldbrandt, M; Christensen, IT; Jørgensen, AS; Ynddal, L; Brand, CL; Bagger, MA; Lau, J Human glucagon receptor antagonists with thiazole cores. A novel series with superior pharmacokinetic properties. J Med Chem 52:2989-3000 (2009) [PubMed]  Article 
Target
Name:
Gastric inhibitory polypeptide receptor
Synonyms:
GIPR | GIPR_HUMAN | Gastric Inhibitory Polypeptide Receptor (GIPR) | Gastric inhibitory polypeptide receptor
Type:
PROTEIN
Mol. Mass.:
53173.82
Organism:
Homo sapiens (Human)
Description:
ChEMBL_1518286
Residue:
466
Sequence:
MTTSPILQLLLRLSLCGLLLQRAETGSKGQTAGELYQRWERYRRECQETLAAAEPPSGLACNGSFDMYVCWDYAAPNATARASCPWYLPWHHHVAAGFVLRQCGSDGQWGLWRDHTQCENPEKNEAFLDQRLILERLQVMYTVGYSLSLATLLLALLILSLFRRLHCTRNYIHINLFTSFMLRAAAILSRDRLLPRPGPYLGDQALALWNQALAACRTAQIVTQYCVGANYTWLLVEGVYLHSLLVLVGGSEEGHFRYYLLLGWGAPALFVIPWVIVRYLYENTQCWERNEVKAIWWIIRTPILMTILINFLIFIRILGILLSKLRTRQMRCRDYRLRLARSTLTLVPLLGVHEVVFAPVTEEQARGALRFAKLGFEIFLSSFQGFLVSVLYCFINKEVQSEIRRGWHHCRLRRSLGEEQRQLPERAFRALPSGSGPGEVPTSRGLSSGTLPGPGNEASRELESYC
  
Inhibitor
Name:
BDBM29130
Synonyms:
thiazole, 27
Type:
Small organic molecule
Emp. Form.:
C28H22ClF3N2O3S
Mol. Mass.:
558.999
SMILES:
OC(=O)CCNC(=O)c1ccc(CC(c2nc(cs2)-c2ccc(cc2)C(F)(F)F)c2ccc(Cl)cc2)cc1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
125I-GIP
Synonyms:
125I-Gastric inhibitory polypeptide | 125I-Glucose-dependent insulinotropic polypeptide
Type:
radiolabeled peptide substrate
Mol. Mass.:
4977.06
Organism:
Sus scrofa (Pig)
Description:
n/a
Residue:
42
Sequence:
YAEGTFISDYSIAMDKIRQQDFVNWLLAQKGKKSDWKHNITQ