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Target
Glucagon receptor
Ligand
BDBM50007239
Substrate
n/a
Meas. Tech.
ChEMBL_1338729 (CHEMBL3242200)
IC50
84±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:
BDBM50007239
Synonyms:
CHEMBL3238226
Type:
Small organic molecule
Emp. Form.:
C33H43ClN8O2
Mol. Mass.:
619.2
SMILES:
CC(C)(C)CC[C@@H](N1C(=O)C(=N[C@@]11CC[C@@H](CC1)C(C)(C)C)c1cncc(Cl)c1)c1ccc(cc1)C(=O)NCc1nn[nH]n1 |r,wU:15.19,6.5,wD:12.13,c:10,(30.07,-58.93,;30.05,-57.39,;28.71,-56.63,;28.71,-58.14,;31.38,-56.6,;31.36,-55.06,;32.68,-54.28,;32.63,-52.74,;33.84,-51.79,;35.32,-52.2,;33.31,-50.34,;31.76,-50.4,;31.35,-51.88,;30.16,-50.89,;28.71,-51.43,;28.45,-52.94,;29.64,-53.93,;31.09,-53.4,;27.01,-53.48,;25.83,-52.49,;25.56,-54.01,;26.75,-54.99,;34.08,-49.01,;35.62,-49.02,;36.4,-47.69,;35.64,-46.35,;34.1,-46.35,;33.33,-45.01,;33.32,-47.68,;34.01,-55.06,;33.98,-56.61,;35.31,-57.39,;36.66,-56.64,;36.68,-55.1,;35.35,-54.32,;37.98,-57.43,;37.96,-58.97,;39.32,-56.68,;40.64,-57.46,;41.99,-56.71,;43.38,-57.34,;44.42,-56.21,;43.67,-54.87,;42.16,-55.17,)|