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Target
Glucagon receptor
Ligand
BDBM50244078
Substrate
n/a
Meas. Tech.
ChEMBL_491826 (CHEMBL945216)
IC50
32±n/a nM
Citation
 Kim, RM; Chang, J; Lins, AR; Brady, E; Candelore, MR; Dallas-Yang, Q; Ding, V; Dragovic, J; Iliff, S; Jiang, G; Mock, S; Qureshi, S; Saperstein, R; Szalkowski, D; Tamvakopoulos, C; Tota, L; Wright, M; Yang, X; Tata, JR; Chapman, K; Zhang, BB; Parmee, ER Discovery of potent, orally active benzimidazole glucagon receptor antagonists. Bioorg Med Chem Lett 18:3701-5 (2008) [PubMed]  Article 
Target
Name:
Glucagon receptor
Synonyms:
GCGR | GL-R | GLR_HUMAN | Glucagon Receptor (GCGR) | Glucagon receptor (GlucR)
Type:
Enzyme
Mol. Mass.:
54026.92
Organism:
Homo sapiens (Human)
Description:
P47871
Residue:
477
Sequence:
MPPCQPQRPLLLLLLLLACQPQVPSAQVMDFLFEKWKLYGDQCHHNLSLLPPPTELVCNRTFDKYSCWPDTPANTTANISCPWYLPWHHKVQHRFVFKRCGPDGQWVRGPRGQPWRDASQCQMDGEEIEVQKEVAKMYSSFQVMYTVGYSLSLGALLLALAILGGLSKLHCTRNAIHANLFASFVLKASSVLVIDGLLRTRYSQKIGDDLSVSTWLSDGAVAGCRVAAVFMQYGIVANYCWLLVEGLYLHNLLGLATLPERSFFSLYLGIGWGAPMLFVVPWAVVKCLFENVQCWTSNDNMGFWWILRFPVFLAILINFFIFVRIVQLLVAKLRARQMHHTDYKFRLAKSTLTLIPLLGVHEVVFAFVTDEHAQGTLRSAKLFFDLFLSSFQGLLVAVLYCFLNKEVQSELRRRWHRWRLGKVLWEERNTSNHRASSSPGHGPPSKELQFGRGGGSQDSSAETPLAGGLPRLAESPF
  
Inhibitor
Name:
BDBM50244078
Synonyms:
CHEMBL502203 | trans-4-[9-tert-Butyl-2-oxo-3-(4-trifluoromethoxy-phenyl)-1,3-diaza-spiro[5.5]undec-1-ylmethyl]-N-(1H-tetrazol-5-yl)-benzamide
Type:
Small organic molecule
Emp. Form.:
C29H34F3N7O3
Mol. Mass.:
585.6206
SMILES:
CC(C)(C)[C@H]1CC[C@]2(CC1)CCN(C(=O)N2Cc1ccc(cc1)C(=O)Nc1nnn[nH]1)c1ccc(OC(F)(F)F)cc1 |r,wU:4.3,wD:7.16,(15.27,-10.56,;16.61,-9.8,;17.38,-11.14,;15.85,-8.46,;17.95,-9.03,;17.95,-7.49,;19.28,-6.73,;20.61,-7.5,;20.62,-9.03,;19.28,-9.8,;20.64,-5.96,;21.98,-5.2,;23.3,-5.98,;23.29,-7.52,;24.62,-8.3,;21.95,-8.27,;21.94,-9.81,;23.27,-10.59,;24.6,-9.82,;25.93,-10.6,;25.92,-12.14,;24.58,-12.91,;23.25,-12.12,;27.25,-12.92,;27.24,-14.46,;28.59,-12.16,;29.92,-12.94,;30.44,-14.39,;31.98,-14.35,;32.42,-12.87,;31.15,-12,;24.65,-5.22,;25.97,-6.01,;27.31,-5.25,;27.32,-3.71,;28.66,-2.95,;29.99,-3.73,;31.31,-4.5,;29.21,-5.06,;30.78,-2.41,;25.98,-2.93,;24.65,-3.69,)|
Structure:
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