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Target
Glucagon receptor
Ligand
BDBM50007231
Substrate
n/a
Meas. Tech.
ChEMBL_1338729 (CHEMBL3242200)
IC50
90±n/a nM
Citation
DeMong, D; Dai, X; Hwa, J; Miller, M; Lin, SI; Kang, L; Stamford, A; Greenlee, W; Yu, W; Wong, M; Lavey, B; Kozlowski, J; Zhou, G; Yang, DY; Patel, B; Soriano, A; Zhai, Y; Sondey, C; Zhang, H; Lachowicz, J; Grotz, D; Cox, K; Morrison, R; Andreani, T; Cao, Y; Liang, M; Meng, T; McNamara, P; Wong, J; Bradley, P; Feng, KI; Belani, J; Chen, P; Dai, P; Gauuan, J; Lin, P; Zhao, H The discovery of N-((2H-tetrazol-5-yl)methyl)-4-((R)-1-((5r,8R)-8-(tert-butyl)-3-(3,5-dichlorophenyl)-2-oxo-1,4-diazaspiro[4.5]dec-3-en-1-yl)-4,4-dimethylpentyl)benzamide (SCH 900822): a potent and selective glucagon receptor antagonist. J Med Chem 57:2601-10 (2014) [PubMed] Article
More Info.:
Target
Name:
Glucagon receptor
Synonyms:
GL-R | GLR_MOUSE | Gcgr
Type:
PROTEIN
Mol. Mass.:
54941.21
Organism:
Mouse
Description:
ChEMBL_1338729
Residue:
485
Sequence:
MPLTQLHCPHLLLLLLVLSCLPEAPSAQVMDFLFEKWKLYSDQCHHNLSLLPPPTELVCNRTFDKYSCWPDTPPNTTANISCPWYLPWYHKVQHRLVFKRCGPDGQWVRGPRGQPWRNASQCQLDDEEIEVQKGVAKMYSSQQVMYTVGYSLSLGALLLALVILLGLRKLHCTRNYIHGNLFASFVLKAGSVLVIDWLLKTRYSQKIGDDLSVSVWLSDGAMAGCRVATVIMQYGIIANYCWLLVEGVYLYSLLSLATFSERSFFSLYLGIGWGAPLLFVIPWVVVKCLFENVQCWTSNDNMGFWWILRIPVFLALLINFFIFVHIIHLLVAKLRAHQMHYADYKFRLARSTLTLIPLLGVHEVVFAFVTDEHAQGTLRSTKLFFDLFLSSFQGLLVAVLYCFLNKEVQAELMRRWRQWQEGKALQEERLASSHGSHMAPAGPCHGDPCEKLQLMSAGSSSGTGCVPSMETSLASSLPRLADSPT
Inhibitor
Name:
BDBM50007231
Synonyms:
CHEMBL3238221
Type:
Small organic molecule
Emp. Form.:
C34H44FN7O2
Mol. Mass.:
601.7573
SMILES:
CC(C)(C)CC[C@@H](N1C(=O)C(=N[C@@]11CC[C@@H](CC1)C(C)(C)C)c1ccc(F)cc1)c1ccc(cc1)C(=O)NCc1nn[nH]n1 |r,wU:15.19,6.5,wD:12.13,c:10,(52.44,-30.45,;52.42,-28.91,;51.08,-28.16,;51.08,-29.67,;53.74,-28.13,;53.72,-26.59,;55.05,-25.8,;54.99,-24.27,;56.21,-23.32,;57.68,-23.73,;55.67,-21.87,;54.13,-21.93,;53.71,-23.41,;52.53,-22.42,;51.08,-22.95,;50.82,-24.47,;52,-25.46,;53.45,-24.92,;49.38,-25,;48.19,-24.02,;47.93,-25.54,;49.12,-26.52,;56.45,-20.54,;57.99,-20.55,;58.77,-19.22,;58.01,-17.88,;58.78,-16.55,;56.46,-17.87,;55.69,-19.2,;56.37,-26.59,;56.35,-28.13,;57.68,-28.92,;59.02,-28.17,;59.04,-26.63,;57.72,-25.84,;60.35,-28.96,;60.33,-30.5,;61.69,-28.2,;63.01,-28.99,;64.35,-28.23,;65.75,-28.87,;66.79,-27.74,;66.04,-26.4,;64.53,-26.7,)|