MK-0893 [Ligand Id: 9135] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1933349 (Mk-0893, Mk0893, MK-0893) |
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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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
