MK-0893 [Ligand Id: 9135] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1933349 (MK-0893, Mk-0893)
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  • GIP receptor/Gastric inhibitory polypeptide receptor in Human [ChEMBL: CHEMBL4383] [GtoPdb: 248] [UniProtKB: P48546]
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  • GLP-1 receptor/Glucagon-like peptide 1 receptor in Human [ChEMBL: CHEMBL1784] [GtoPdb: 249] [UniProtKB: P43220]
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  • glucagon receptor/Glucagon receptor in Human [ChEMBL: CHEMBL1985] [GtoPdb: 251] [UniProtKB: P47871]
  • glucagon receptor/Glucagon receptor in Mouse [ChEMBL: CHEMBL4773] [GtoPdb: 251] [UniProtKB: Q61606]
  • glucagon receptor/Glucagon receptor in Rat [ChEMBL: CHEMBL4720] [GtoPdb: 251] [UniProtKB: P30082]
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  • VPAC1 receptor/Vasoactive intestinal polypeptide receptor 1 in Human [ChEMBL: CHEMBL5144] [GtoPdb: 371] [UniProtKB: P32241]
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  • VPAC2 receptor/Vasoactive intestinal polypeptide receptor 2 in Human [ChEMBL: CHEMBL4532] [GtoPdb: 372] [UniProtKB: P41587]
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  • PAC1 receptor in Human [GtoPdb: 370] [UniProtKB: P41586]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Dual specificity protein phosphatase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2157858] [UniProtKB: Q05923]
ChEMBL Antagonist activity at human PAC1 expressed in mouse HIN 3T3 cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter F 5.04 pIC50 9200 nM IC50 J. Med. Chem. (2012) 55: 6137-6148 [PMID:22708876]
GIP receptor/Gastric inhibitory polypeptide receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4383] [GtoPdb: 248] [UniProtKB: P48546]
GtoPdb - - 5.99 pIC50 1020 nM IC50 J Med Chem (2012) 55: 6137-48 [PMID:22708876]
ChEMBL Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter F 5.99 pIC50 1019 nM IC50 J. Med. Chem. (2012) 55: 6137-6148 [PMID:22708876]
GLP-1 receptor/Glucagon-like peptide 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1784] [GtoPdb: 249] [UniProtKB: P43220]
ChEMBL Antagonist activity at human GLP1R expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter F 5 pIC50 >10000 nM IC50 J. Med. Chem. (2012) 55: 6137-6148 [PMID:22708876]
glucagon receptor/Glucagon receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1985] [GtoPdb: 251] [UniProtKB: P47871]
ChEMBL Displacement of [125I]Glucagon-Cex from human GCGR B 7.15 pKi 70 nM Ki Bioorg. Med. Chem. Lett. (2012) 22: 415-420 [PMID:22119466]
ChEMBL Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay F 7.1 pIC50 80 nM IC50 Bioorg Med Chem (2018) 26: 1896-1908 [PMID:29523469]
ChEMBL Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis B 7.7 pIC50 20 nM IC50 Bioorg Med Chem (2018) 26: 1896-1908 [PMID:29523469]
ChEMBL Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter F 7.8 pIC50 15.7 nM IC50 J. Med. Chem. (2012) 55: 6137-6148 [PMID:22708876]
GtoPdb - - 8.18 pIC50 6.6 nM IC50 J Med Chem (2012) 55: 6137-48 [PMID:22708876]
ChEMBL Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay B 8.18 pIC50 6.6 nM IC50 J. Med. Chem. (2012) 55: 6137-6148 [PMID:22708876]
glucagon receptor/Glucagon receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4773] [GtoPdb: 251] [UniProtKB: Q61606]
ChEMBL Antagonist activity at mouse GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter F 6.91 pIC50 122 nM IC50 J. Med. Chem. (2012) 55: 6137-6148 [PMID:22708876]
glucagon receptor/Glucagon receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4720] [GtoPdb: 251] [UniProtKB: P30082]
ChEMBL Antagonist activity at rat GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter F 6.14 pIC50 727 nM IC50 J. Med. Chem. (2012) 55: 6137-6148 [PMID:22708876]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Binding affinity to human ERG B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2012) 55: 6137-6148 [PMID:22708876]
Uncharacterized protein in Rhesus macaque (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2157859] [UniProtKB: A0A1D5QZY8]
ChEMBL Antagonist activity at rhesus monkey GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter F 7.26 pIC50 55.5 nM IC50 J. Med. Chem. (2012) 55: 6137-6148 [PMID:22708876]
Uncharacterized protein in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1649060] [UniProtKB: E2R517]
ChEMBL Antagonist activity at dog GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter F 6.98 pIC50 104.5 nM IC50 J. Med. Chem. (2012) 55: 6137-6148 [PMID:22708876]
VPAC1 receptor/Vasoactive intestinal polypeptide receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5144] [GtoPdb: 371] [UniProtKB: P32241]
ChEMBL Antagonist activity at human VPAC1 expressed in HT-29 cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter F 4.94 pIC50 11580 nM IC50 J. Med. Chem. (2012) 55: 6137-6148 [PMID:22708876]
VPAC2 receptor/Vasoactive intestinal polypeptide receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4532] [GtoPdb: 372] [UniProtKB: P41587]
ChEMBL Antagonist activity at human VPAC2 expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter F 4.89 pIC50 12800 nM IC50 J. Med. Chem. (2012) 55: 6137-6148 [PMID:22708876]
PAC1 receptor in Human [GtoPdb: 370] [UniProtKB: P41586]
GtoPdb - - 5.04 pIC50 9200 nM IC50 J Med Chem (2012) 55: 6137-48 [PMID:22708876]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]