Ki Summary

Reaction Details

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Target

Glucagon receptor

Ligand

BDBM50244235

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_491826 (CHEMBL945216)

IC50

2±n/a nM

Citation

Kim, RM; Chang, J; Lins, AR; Brady, E; Candelore, MR; Dallas-Yang, Q; Ding, V; Dragovic, J; Iliff, S; Jiang, G; Mock, S; Qureshi, S; Saperstein, R; Szalkowski, D; Tamvakopoulos, C; Tota, L; Wright, M; Yang, X; Tata, JR; Chapman, K; Zhang, BB; Parmee, ER Discovery of potent, orally active benzimidazole glucagon receptor antagonists. Bioorg Med Chem Lett18:3701-5 (2008) [PubMed] Article

More Info.:

Get all data from this article, Assay Method

Glucagon receptor

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:

MPPCQPQRPLLLLLLLLACQPQVPSAQVMDFLFEKWKLYGDQCHHNLSLLPPPTELVCNR
TFDKYSCWPDTPANTTANISCPWYLPWHHKVQHRFVFKRCGPDGQWVRGPRGQPWRDASQ
CQMDGEEIEVQKEVAKMYSSFQVMYTVGYSLSLGALLLALAILGGLSKLHCTRNAIHANL
FASFVLKASSVLVIDGLLRTRYSQKIGDDLSVSTWLSDGAVAGCRVAAVFMQYGIVANYC
WLLVEGLYLHNLLGLATLPERSFFSLYLGIGWGAPMLFVVPWAVVKCLFENVQCWTSNDN
MGFWWILRFPVFLAILINFFIFVRIVQLLVAKLRARQMHHTDYKFRLAKSTLTLIPLLGV
HEVVFAFVTDEHAQGTLRSAKLFFDLFLSSFQGLLVAVLYCFLNKEVQSELRRRWHRWRL
GKVLWEERNTSNHRASSSPGHGPPSKELQFGRGGGSQDSSAETPLAGGLPRLAESPF

BDBM50244235

n/a

Name

BDBM50244235

Synonyms:

CHEMBL480692 | trans-4-(((4-tert-butylcyclohexyl)(1-methyl-5-propoxy-1H-benzo[d]imidazol-2-yl)amino)methyl)-N-(1H-tetrazol-5-yl)benzamide

Type

Small organic molecule

Emp. Form.

C30H40N8O2

Mol. Mass.

544.691

SMILES

CCCOc1ccc2n(C)c(nc2c1)N(Cc1ccc(cc1)C(=O)Nc1nnn[nH]1)[C@H]1CC[C@@H](CC1)C(C)(C)C |r,wU:30.33,wD:33.40,(15,-40.17,;14.2,-41.49,;14.94,-42.84,;14.14,-44.16,;14.88,-45.51,;14.07,-46.83,;14.81,-48.17,;16.34,-48.21,;17.35,-49.38,;16.57,-50.71,;18.77,-48.79,;18.65,-47.25,;17.15,-46.9,;16.41,-45.55,;20.1,-49.57,;20.09,-51.11,;21.42,-51.88,;22.75,-51.12,;24.08,-51.89,;24.07,-53.43,;22.73,-54.2,;21.4,-53.42,;25.4,-54.21,;25.39,-55.75,;26.74,-53.45,;28.07,-54.23,;28.59,-55.68,;30.13,-55.64,;30.57,-54.16,;29.3,-53.29,;21.43,-48.8,;21.43,-47.27,;22.78,-46.51,;24.11,-47.29,;24.09,-48.83,;22.76,-49.58,;25.45,-46.53,;26.77,-45.75,;26.22,-47.86,;24.68,-45.19,)|

Structure