omarigliptin [Ligand Id: 8402] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2105762 (MK-3102, Omarigliptin)
  • Dipeptidyl-peptidase 7/Dipeptidyl peptidase II in Human [ChEMBL: CHEMBL3976] [GtoPdb: 1605] [UniProtKB: Q9UHL4]
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  • dipeptidyl peptidase 4/Dipeptidyl peptidase IV in Human [ChEMBL: CHEMBL284] [GtoPdb: 1612] [UniProtKB: P27487]
  • dipeptidyl peptidase 4/Dipeptidyl peptidase IV in Mouse [ChEMBL: CHEMBL3883] [GtoPdb: 1612] [UniProtKB: P28843]
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  • dipeptidyl peptidase 9/Dipeptidyl peptidase IX in Human [ChEMBL: CHEMBL4793] [GtoPdb: 2357] [UniProtKB: Q86TI2]
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  • dipeptidyl peptidase 8/Dipeptidyl peptidase VIII in Human [ChEMBL: CHEMBL4657] [GtoPdb: 2356] [UniProtKB: Q6V1X1]
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  • fibroblast activation protein alpha/Fibroblast activation protein alpha in Human [ChEMBL: CHEMBL4683] [GtoPdb: 2365] [UniProtKB: Q12884]
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  • prolyl endopeptidase/Prolyl endopeptidase in Human [ChEMBL: CHEMBL3202] [GtoPdb: 2395] [UniProtKB: P48147]
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  • Nav1.5/Sodium channel protein type V alpha subunit in Human [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
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  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]