omarigliptin [Ligand Id: 8402] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2105762 (MK-3102, Omarigliptin, Omarigliptina, Omarigliptine) |
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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] |
| ChEMBL | Inhibition of DPP-4 (unknown origin) | B | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (2023) 66: 11593-11631 [PMID:37647598] |
| ChEMBL | Inhibition of human recombinant DPP-4 (1 to 530 residues) using Gly-Pro-AMC as substrate preincubated for 30 mins followed by substrate addition measured after 5 mins by CF assay | B | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (2023) 66: 11593-11631 [PMID:37647598] |
| ChEMBL | Inhibition of DPP-4 (unknown origin) | B | 8.6 | pEC50 | 2.5 | nM | EC50 | J Med Chem (2023) 66: 11593-11631 [PMID:37647598] |
| 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 35:
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]
