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Target
Glucagon receptor
Ligand
BDBM50007210
Substrate
n/a
Meas. Tech.
ChEMBL_1338729 (CHEMBL3242200)
IC50
370±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:
BDBM50007210
Synonyms:
CHEMBL3237922
Type:
Small organic molecule
Emp. Form.:
C30H35Cl2N7O2
Mol. Mass.:
596.551
SMILES:
CC[C@@H](N1C(=O)C(=N[C@@]11CC[C@@H](CC1)C(C)(C)C)c1cc(Cl)cc(Cl)c1)c1ccc(cc1)C(=O)NCc1nn[nH]n1 |r,wU:11.15,2.1,wD:8.9,c:6,(32.2,-13.03,;32.18,-11.49,;33.51,-10.71,;33.45,-9.17,;34.67,-8.22,;36.14,-8.63,;34.13,-6.77,;32.59,-6.83,;32.17,-8.31,;30.99,-7.32,;29.54,-7.86,;29.28,-9.37,;30.46,-10.36,;31.91,-9.83,;27.84,-9.91,;26.65,-8.92,;26.39,-10.44,;27.58,-11.42,;34.91,-5.44,;34.15,-4.11,;34.92,-2.78,;34.16,-1.44,;36.47,-2.78,;37.23,-4.12,;38.77,-4.13,;36.45,-5.46,;34.83,-11.49,;34.81,-13.04,;36.14,-13.82,;37.48,-13.07,;37.5,-11.53,;36.18,-10.75,;38.81,-13.86,;38.79,-15.4,;40.14,-13.11,;41.47,-13.89,;42.81,-13.14,;44.21,-13.77,;45.25,-12.64,;44.5,-11.3,;42.99,-11.6,)|