Reaction Details |
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Target | Glucagon receptor |
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Ligand | BDBM50433577 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_960258 (CHEMBL2382751) |
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Ki | 14±n/a nM |
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Citation | Guzman-Perez, A; Pfefferkorn, JA; Lee, EC; Stevens, BD; Aspnes, GE; Bian, J; Didiuk, MT; Filipski, KJ; Moore, D; Perreault, C; Sammons, MF; Tu, M; Brown, J; Atkinson, K; Litchfield, J; Tan, B; Samas, B; Zavadoski, WJ; Salatto, CT; Treadway, J The design and synthesis of a potent glucagon receptor antagonist with favorable physicochemical and pharmacokinetic properties as a candidate for the treatment of type 2 diabetes mellitus. Bioorg Med Chem Lett23:3051-8 (2013) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Glucagon receptor |
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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
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BDBM50433577 |
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n/a |
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Name | BDBM50433577 |
Synonyms: | CHEMBL2381848 |
Type | Small organic molecule |
Emp. Form. | C26H28F3N3O4 |
Mol. Mass. | 503.5134 |
SMILES | CCC[C@H](Oc1cc(C)c(c(C)c1)-n1cc(cn1)C(F)(F)F)c1ccc(cc1)C(=O)NCCC(O)=O |r| |
Structure |
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