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Target
Glucagon receptor
Ligand
BDBM50007218
Substrate
n/a
Meas. Tech.
ChEMBL_1338729 (CHEMBL3242200)
IC50
280±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:
BDBM50007218
Synonyms:
CHEMBL3237928
Type:
Small organic molecule
Emp. Form.:
C33H41Cl2N7O2
Mol. Mass.:
638.63
SMILES:
CC(C)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:14.18,5.4,wD:11.12,c:9,(30.64,-43.26,;30.62,-41.72,;29.28,-40.97,;31.95,-40.94,;31.93,-39.4,;33.25,-38.61,;33.2,-37.07,;34.41,-36.12,;35.89,-36.54,;33.88,-34.68,;32.34,-34.74,;31.92,-36.21,;30.73,-35.23,;29.29,-35.76,;29.02,-37.28,;30.21,-38.26,;31.66,-37.73,;27.59,-37.81,;26.4,-36.82,;26.14,-38.34,;27.32,-39.33,;34.66,-33.35,;33.89,-32.01,;34.67,-30.68,;33.9,-29.34,;36.21,-30.69,;36.97,-32.03,;38.51,-32.04,;36.2,-33.36,;34.58,-39.39,;34.56,-40.94,;35.88,-41.72,;37.23,-40.97,;37.25,-39.43,;35.92,-38.65,;38.55,-41.76,;38.53,-43.3,;39.89,-41.01,;41.22,-41.79,;42.56,-41.04,;43.95,-41.68,;45,-40.54,;44.24,-39.2,;42.73,-39.51,)|