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Target
Glucagon receptor
Ligand
BDBM50007440
Substrate
n/a
Meas. Tech.
ChEMBL_1338729 (CHEMBL3242200)
IC50
400±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:
BDBM50007440
Synonyms:
CHEMBL3237917
Type:
Small organic molecule
Emp. Form.:
C29H33Cl2N7O2
Mol. Mass.:
582.524
SMILES:
C[C@@H](N1C(=O)C(=N[C@@]11CC[C@@H](CC1)C(C)(C)C)c1cc(Cl)cc(Cl)c1)c1ccc(cc1)C(=O)NCc1nnn[nH]1 |r,wU:10.14,1.0,wD:7.8,c:5,(28.51,-39.62,;29.84,-38.83,;29.78,-37.3,;31,-36.35,;32.47,-36.76,;30.46,-34.9,;28.92,-34.96,;28.5,-36.44,;27.32,-35.45,;25.87,-35.98,;25.61,-37.5,;26.79,-38.49,;28.24,-37.95,;24.17,-38.03,;22.98,-37.05,;22.72,-38.56,;23.91,-39.55,;31.24,-33.57,;30.48,-32.23,;31.25,-30.9,;30.49,-29.57,;32.8,-30.91,;33.56,-32.25,;35.1,-32.26,;32.78,-33.58,;31.16,-39.62,;31.14,-41.16,;32.47,-41.95,;33.81,-41.19,;33.83,-39.66,;32.51,-38.87,;35.14,-41.99,;35.11,-43.52,;36.47,-41.23,;37.8,-42.02,;39.14,-41.26,;40.54,-41.9,;41.58,-40.77,;40.82,-39.42,;39.32,-39.73,)|