Ki Summary

Reaction Details

Report a problem with these data

Target

Glucagon receptor

Ligand

BDBM50007232

Substrate

n/a

Meas. Tech.

ChEMBL_1338728 (CHEMBL3242199)

IC50

13±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.:

Get all data from this article, Assay Method

Target

Name:

Glucagon receptor

Synonyms:

GCGR | GL-R | GLR_HUMAN | Glucagon Receptor (GCGR) | Glucagon receptor (GlucR)

Type:

Enzyme

Mol. Mass.:

54026.92

Organism:

Homo sapiens (Human)

Description:

P47871

Residue:

477

Sequence:

MPPCQPQRPLLLLLLLLACQPQVPSAQVMDFLFEKWKLYGDQCHHNLSLLPPPTELVCNRTFDKYSCWPDTPANTTANISCPWYLPWHHKVQHRFVFKRCGPDGQWVRGPRGQPWRDASQCQMDGEEIEVQKEVAKMYSSFQVMYTVGYSLSLGALLLALAILGGLSKLHCTRNAIHANLFASFVLKASSVLVIDGLLRTRYSQKIGDDLSVSTWLSDGAVAGCRVAAVFMQYGIVANYCWLLVEGLYLHNLLGLATLPERSFFSLYLGIGWGAPMLFVVPWAVVKCLFENVQCWTSNDNMGFWWILRFPVFLAILINFFIFVRIVQLLVAKLRARQMHHTDYKFRLAKSTLTLIPLLGVHEVVFAFVTDEHAQGTLRSAKLFFDLFLSSFQGLLVAVLYCFLNKEVQSELRRRWHRWRLGKVLWEERNTSNHRASSSPGHGPPSKELQFGRGGGSQDSSAETPLAGGLPRLAESPF

Inhibitor

Name:

BDBM50007232

Synonyms:

CHEMBL3238222

Type:

Small organic molecule

Emp. Form.:

C34H43F2N7O2

Mol. Mass.:

619.7477

SMILES:

CC(C)(C)CC[C@@H](N1C(=O)C(=N[C@@]11CC[C@@H](CC1)C(C)(C)C)c1ccc(F)c(F)c1)c1ccc(cc1)C(=O)NCc1nn[nH]n1 |r,wU:15.19,6.5,wD:12.13,c:10,(5.5,-43.18,;5.48,-41.64,;4.14,-40.89,;4.15,-42.4,;6.81,-40.86,;6.79,-39.32,;8.11,-38.53,;8.06,-37,;9.27,-36.05,;10.75,-36.46,;8.74,-34.6,;7.19,-34.66,;6.78,-36.14,;5.59,-35.15,;4.14,-35.68,;3.88,-37.2,;5.07,-38.19,;6.52,-37.65,;2.44,-37.73,;1.26,-36.75,;1,-38.27,;2.18,-39.25,;9.51,-33.27,;8.75,-31.93,;9.53,-30.6,;11.07,-30.61,;11.85,-29.28,;11.83,-31.95,;13.37,-31.96,;11.06,-33.28,;9.44,-39.32,;9.42,-40.86,;10.74,-41.65,;12.09,-40.9,;12.11,-39.36,;10.78,-38.57,;13.41,-41.69,;13.39,-43.23,;14.75,-40.93,;16.08,-41.72,;17.42,-40.96,;18.81,-41.6,;19.86,-40.47,;19.1,-39.13,;17.59,-39.43,)|

Structure: