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ChEMBL ligand: CHEMBL2105762 (MK-3102, Omarigliptin) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Dipeptidyl-peptidase 7/Dipeptidyl peptidase II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3976] [GtoPdb: 1605] [UniProtKB: Q9UHL4] | ||||||||
ChEMBL | Inhibition of N-terminal FLAG tagged human QPP expressed in Sf9 cells using Nle-Pro-AMC substrate after 30 mins by plate reader analysis | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 5767-5771 [PMID:26546218] |
ChEMBL | Inhibition of QPP (unknown origin) | B | 4.17 | pIC50 | >67000 | nM | IC50 | J Med Chem (2014) 57: 3205-3212 [PMID:24660890] |
dipeptidyl peptidase 4/Dipeptidyl peptidase IV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL284] [GtoPdb: 1612] [UniProtKB: P27487] | ||||||||
ChEMBL | Binding affinity to DPP4 (unknown origin) assessed as dissociation constant by SPR assay | B | 8.56 | pKd | 2.75 | nM | Kd | J Med Chem (2016) 59: 6772-6790 [PMID:27396490] |
ChEMBL | Binding affinity to DPP4 (unknown origin) expressed in baculovirus expressing system | B | 8.56 | pKd | 2.75 | nM | Kd | J Med Chem (2019) 62: 2348-2361 [PMID:30694668] |
ChEMBL | Competitive reversible inhibition of DPP4 (unknown origin) | B | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (2014) 57: 3205-3212 [PMID:24660890] |
GtoPdb | - | - | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (2014) 57: 3205-12 [PMID:24660890] |
ChEMBL | Inhibition of human recombinant DPP4 incubated for 15 mins using Gly-Pro-7-AMC substrate | B | 8.51 | pIC50 | 3.1 | nM | IC50 | J Med Chem (2020) 63: 7108-7126 [PMID:32452679] |
ChEMBL | Inhibition of recombinant human DPP4 expressed in Sf9 cells using Gly-Pro-AMC substrate after 30 mins by plate reader analysis | B | 8.59 | pIC50 | 2.6 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 5767-5771 [PMID:26546218] |
ChEMBL | Inhibition of DPP4 (unknown origin) expressed in Sf9 cells using Gly-Pro-AMC substrate | B | 8.65 | pIC50 | 2.22 | nM | IC50 | J Med Chem (2016) 59: 6772-6790 [PMID:27396490] |
ChEMBL | Competitive reversible inhibition of DPP4 (unknown origin) | B | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (2014) 57: 3205-3212 [PMID:24660890] |
dipeptidyl peptidase 4/Dipeptidyl peptidase IV in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3883] [GtoPdb: 1612] [UniProtKB: P28843] | ||||||||
ChEMBL | Inhibition of DPP4 in mouse plasma | B | 7.36 | pIC50 | 43.9 | nM | IC50 | J Med Chem (2014) 57: 3205-3212 [PMID:24660890] |
dipeptidyl peptidase 9/Dipeptidyl peptidase IX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4793] [GtoPdb: 2357] [UniProtKB: Q86TI2] | ||||||||
ChEMBL | Inhibition of DPP9 (unknown origin) | B | 4.17 | pIC50 | >67000 | nM | IC50 | J Med Chem (2014) 57: 3205-3212 [PMID:24660890] |
dipeptidyl peptidase 8/Dipeptidyl peptidase VIII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4657] [GtoPdb: 2356] [UniProtKB: Q6V1X1] | ||||||||
ChEMBL | Inhibition of C-terminal His-tagged DPP8 (unknown origin) expressed in COS7 cells using H-Ala-Pro-pNA substrate preincubated for 15 mins | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 5767-5771 [PMID:26546218] |
ChEMBL | Inhibition of DPP8 (unknown origin) | B | 4.17 | pIC50 | >67000 | nM | IC50 | J Med Chem (2014) 57: 3205-3212 [PMID:24660890] |
fibroblast activation protein alpha/Fibroblast activation protein alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4683] [GtoPdb: 2365] [UniProtKB: Q12884] | ||||||||
ChEMBL | Inhibition of FAP (unknown origin) | B | 4.17 | pIC50 | >67000 | nM | IC50 | J Med Chem (2014) 57: 3205-3212 [PMID:24660890] |
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
ChEMBL | Inhibition of human ERG assessed as reduction in IKr current | B | 4.41 | pIC50 | 39000 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 5767-5771 [PMID:26546218] |
ChEMBL | Inhibition of human ERG by MK-499 displacement binding analysis | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2014) 57: 3205-3212 [PMID:24660890] |
prolyl endopeptidase/Prolyl endopeptidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3202] [GtoPdb: 2395] [UniProtKB: P48147] | ||||||||
ChEMBL | Inhibition of PEP (unknown origin) | B | 4.17 | pIC50 | >67000 | nM | IC50 | J Med Chem (2014) 57: 3205-3212 [PMID:24660890] |
Prolyl endopeptidase FAP in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3734641] [UniProtKB: A5D7B7] | ||||||||
ChEMBL | Inhibition of bovine serum FAP | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 5767-5771 [PMID:26546218] |
Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524] | ||||||||
ChEMBL | Inhibition of Nav1.5 (unknown origin) | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2014) 57: 3205-3212 [PMID:24660890] |
Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936] | ||||||||
ChEMBL | Inhibition of Cav1.2 (unknown origin) | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2014) 57: 3205-3212 [PMID:24660890] |
ChEMBL | Inhibition of potassium channel Cav1.2 (unknown origin) | B | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 5767-5771 [PMID:26546218] |
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]