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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
