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Target
Glucagon receptor
Ligand
BDBM50007212
Substrate
n/a
Meas. Tech.
ChEMBL_1338729 (CHEMBL3242200)
IC50
420±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:
Mus musculus
Description:
ChEMBL_1338729
Residue:
485
Sequence:
MPLTQLHCPHLLLLLLVLSCLPEAPSAQVMDFLFEKWKLYSDQCHHNLSLLPPPTELVCNRTFDKYSCWPDTPPNTTANISCPWYLPWYHKVQHRLVFKRCGPDGQWVRGPRGQPWRNASQCQLDDEEIEVQKGVAKMYSSQQVMYTVGYSLSLGALLLALVILLGLRKLHCTRNYIHGNLFASFVLKAGSVLVIDWLLKTRYSQKIGDDLSVSVWLSDGAMAGCRVATVIMQYGIIANYCWLLVEGVYLYSLLSLATFSERSFFSLYLGIGWGAPLLFVIPWVVVKCLFENVQCWTSNDNMGFWWILRIPVFLALLINFFIFVHIIHLLVAKLRAHQMHYADYKFRLARSTLTLIPLLGVHEVVFAFVTDEHAQGTLRSTKLFFDLFLSSFQGLLVAVLYCFLNKEVQAELMRRWRQWQEGKALQEERLASSHGSHMAPAGPCHGDPCEKLQLMSAGSSSGTGCVPSMETSLASSLPRLADSPT
Inhibitor
Name:
BDBM50007212
Synonyms:
CHEMBL3237924
Type:
Small organic molecule
Emp. Form.:
C32H39Cl2N7O2
Mol. Mass.:
624.604
SMILES:
CCCC[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:13.17,4.3,wD:10.11,c:8,(5.36,-28.28,;5.34,-26.74,;6.67,-25.96,;6.65,-24.42,;7.97,-23.63,;7.92,-22.1,;9.13,-21.15,;10.61,-21.56,;8.6,-19.7,;7.05,-19.76,;6.64,-21.24,;5.45,-20.25,;4,-20.78,;3.74,-22.3,;4.93,-23.29,;6.38,-22.75,;2.3,-22.83,;1.12,-21.85,;.86,-23.37,;2.04,-24.35,;9.37,-18.37,;8.61,-17.03,;9.39,-15.7,;8.62,-14.37,;10.93,-15.71,;11.69,-17.05,;13.23,-17.06,;10.92,-18.38,;9.3,-24.42,;9.28,-25.96,;10.6,-26.75,;11.95,-26,;11.97,-24.46,;10.64,-23.67,;13.27,-26.79,;13.25,-28.33,;14.61,-26.03,;15.94,-26.82,;17.28,-26.06,;18.67,-26.7,;19.72,-25.57,;18.96,-24.23,;17.45,-24.53,)|