sitagliptin [Ligand Id: 6286] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1422 (Januvia, LEZ-763, LEZ763, MK-0431, Sitagliptin) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Aminopeptidase N in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1907] [GtoPdb: 1560] [UniProtKB: P15144] | ||||||||
| ChEMBL | Inhibition of APN (unknown origin) | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2313-2318 [PMID:28442252] |
| Angiotensin-converting enzyme in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1808] [GtoPdb: 1613] [UniProtKB: P12821] | ||||||||
| ChEMBL | Inhibition of human plasma ACE | B | 4.96 | pIC50 | 11000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2313-2318 [PMID:28442252] |
| Dipeptidyl peptidase 9 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295538] [UniProtKB: E1BI31] | ||||||||
| ChEMBL | Inhibition of bovine DPP9 | B | 4 | pIC50 | >100000 | nM | IC50 | Eur J Med Chem (2017) 139: 482-491 [PMID:28826083] |
| Dipeptidyl-peptidase 7/Dipeptidyl peptidase II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3976] [GtoPdb: 1605] [UniProtKB: Q9UHL4] | ||||||||
| ChEMBL | Inhibition of DPP2 (unknown origin) | B | 4 | pIC50 | >100000 | nM | IC50 | Eur J Med Chem (2017) 139: 482-491 [PMID:28826083] |
| ChEMBL | Inhibition of QPP | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 3877-3879 [PMID:17502141] |
| ChEMBL | Inhibition of DPP2 (unknown origin) | B | 4 | pIC50 | >100000 | nM | IC50 | Medchemcomm (2014) 5: 1700-1707 |
| ChEMBL | Inhibition of DPP2 (unknown origin) | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2313-2318 [PMID:28442252] |
| ChEMBL | Inhibition of QPP | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 3384-3387 [PMID:17433672] |
| ChEMBL | Inhibition of DPP2 | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 4154-4158 [PMID:18556199] |
| ChEMBL | Inhibition of DPP2 | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3596-3600 [PMID:20483603] |
| ChEMBL | Inhibition of human recombinant His-tagged DPP2 expressed in insect cells | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2010) 53: 6572-6583 [PMID:20718420] |
| ChEMBL | Inhibition of QPP | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1880-1886 [PMID:21320777] |
| ChEMBL | Inhibition of DPP2 | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2011) 54: 5737-5746 [PMID:21711053] |
| ChEMBL | Inhibition of human seminal plasma DPP2 assessed as pNA release from Lys-Ala-p-nitroanilide substrate pre-incubated with enzyme for 15 min prior to substrate addition by fluorescence technique | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 3412-3417 [PMID:22525314] |
| ChEMBL | Inhibition of human DPP2 using Lys-Ala-AMC as substrate by fluorimetric analysis | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem (2012) 20: 5864-5883 [PMID:22938786] |
| ChEMBL | Inhibition of recombinant his6-tagged DPP7 (unknown origin) using Nle-Pro-AMC as substrate by continuous fluorometric method | B | 4.22 | pIC50 | 59830 | nM | IC50 | Bioorg Med Chem (2014) 22: 6684-6693 [PMID:25457126] |
| ChEMBL | Inhibition of DPP2 | B | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 1908-1912 [PMID:19269819] |
| ChEMBL | Inhibition of human DPP2 | B | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem (2009) 17: 2388-2399 [PMID:19261480] |
| Dipeptidyl peptidase IV in Porphyromonas gingivalis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295559] [UniProtKB: O31048] | ||||||||
| ChEMBL | Inhibition of Porphyromonas gingivalis N-terminal His-tagged DPP4 expressed in Escherichia coli using Gly-Pro-p-nitroanilide as substrate | B | 4.74 | pIC50 | 18000 | nM | IC50 | Eur J Med Chem (2017) 139: 482-491 [PMID:28826083] |
| dipeptidyl peptidase 4/Dipeptidyl peptidase IV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL284] [GtoPdb: 1612] [UniProtKB: P27487] | ||||||||
| ChEMBL | Binding affinity to human recombinant DPP4 (39 to 766 residues) at 5 uM by isothermal titration calorimetry | B | 7.87 | pKd | 13.5 | nM | Kd | J Med Chem (2016) 59: 7466-7477 [PMID:27438064] |
| ChEMBL | Binding affinity to DPP4 (unknown origin) assessed as dissociation constant by SPR assay | B | 7.9 | pKd | 12.7 | nM | Kd | J Med Chem (2016) 59: 6772-6790 [PMID:27396490] |
| ChEMBL | Binding affinity to DPP4 (unknown origin) expressed in baculovirus expressing system | B | 7.9 | pKd | 12.7 | nM | Kd | J Med Chem (2019) 62: 2348-2361 [PMID:30694668] |
| ChEMBL | Binding affinity to human recombinant DPP4 (39 to 766 residues) by surface plasmon resonance analysis | B | 8.28 | pKd | 5.3 | nM | Kd | J Med Chem (2016) 59: 7466-7477 [PMID:27438064] |
| ChEMBL | Inhibition of human DPP-4 using Ala-Pro-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 5 to 10 mins by fluorescence assay | B | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 3731-3735 [PMID:30343953] |
| ChEMBL | Inhibition of DPP4 in human Caco-2 cells after 60 mins by fluorimetry assay | B | 6.96 | pIC50 | 110 | nM | IC50 | Eur J Med Chem (2008) 43: 1889-1902 [PMID:18243422] |
| ChEMBL | Inhibition of DPP4 in presence of 50% rat serum | B | 7.34 | pIC50 | 46 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3596-3600 [PMID:20483603] |
| ChEMBL | Inhibition of DPP4 | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 4154-4158 [PMID:18556199] |
| ChEMBL | Inhibition of human DPP4 | B | 7.4 | pIC50 | 40 | nM | IC50 | Eur J Med Chem (2017) 139: 482-491 [PMID:28826083] |
| ChEMBL | Inhibition of DPP4 | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2011) 54: 5737-5746 [PMID:21711053] |
| ChEMBL | Inhibition of human seminal plasma DPP4 assessed as pNA release from Gly-Pro-p-nitroanilide substrate pre-incubated with enzyme for 15 min prior to substrate addition by fluorescence technique | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 3412-3417 [PMID:22525314] |
| ChEMBL | Inhibition of human recombinant C-terminal 6His-tagged DPP-4 expressed in insect cells incubated for 30 mins by TPE-KFPE fluorescent probe-based assay | B | 7.42 | pIC50 | 37.96 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2131-2135 [PMID:29773502] |
| ChEMBL | Inhibition of human DPP4 | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem (2009) 17: 2388-2399 [PMID:19261480] |
| ChEMBL | Inhibition of DPP4 | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 1908-1912 [PMID:19269819] |
| ChEMBL | Inhibition of DPP4 | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3596-3600 [PMID:20483603] |
| ChEMBL | Inhibition of human recombinant DPP4 pre-incubated with compound for 15 mins before substrate addition by luminescence assay | B | 7.54 | pIC50 | 29 | nM | IC50 | ACS Med Chem Lett (2014) 5: 921-926 [PMID:25147615] |
| ChEMBL | Inhibition of human purified His-tagged DPP-4 assessed as cleavage of substrate using Gly-Pro-AMC chromogenic substrate after 60 mins by fluorescence spectrophotometry | B | 7.61 | pIC50 | 24.83 | nM | IC50 | Bioorg Med Chem (2013) 21: 5679-5687 [PMID:23938053] |
| ChEMBL | Inhibition of human recombinant His-tagged DPP4 expressed in insect cells | B | 7.64 | pIC50 | 23 | nM | IC50 | J Med Chem (2010) 53: 6572-6583 [PMID:20718420] |
| ChEMBL | Inhibition of human recombinant DPP4 using H-Gly-Pro-AMC substrate incubated for 15 mins by fluorescent AMC release assay | B | 7.66 | pIC50 | 22 | nM | IC50 | ACS Med Chem Lett (2015) 6: 324-328 [PMID:25815154] |
| ChEMBL | Inhibition of human recombinant DPP4 after 60 mins by fluorescence plate reader | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1366-1370 [PMID:21306895] |
| ChEMBL | Inhibition of recombinant his6-tagged DPP4 (unknown origin) expressed in baculovirus expression system using Ala-pro-AMC as substrate by fluorometric analysis | B | 7.7 | pIC50 | 20 | nM | IC50 | Eur J Med Chem (2014) 75: 111-122 [PMID:24531224] |
| ChEMBL | Inhibition of human plasma DPP4 | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2313-2318 [PMID:28442252] |
| ChEMBL | Inhibition of human recombinant DPP4 expressed in baculovirus expression system using Ala-Pro-AMC as substrate by continuous fluorometric assay | B | 7.7 | pIC50 | 20 | nM | IC50 | Eur J Med Chem (2014) 86: 242-256 [PMID:25164763] |
| ChEMBL | Inhibition of human recombinant his6-tagged DPP4 using Ala-Pro-AMC as substrate by continuous fluorometric method | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem (2014) 22: 6684-6693 [PMID:25457126] |
| ChEMBL | Inhibition of human DPP4 assessed as hydrolytic reaction of Ala-Pro-AMC | B | 7.71 | pIC50 | 19.4 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1731-1735 [PMID:21334204] |
| ChEMBL | Inhibition of DPP4 in human Caco2 cells using H-Ala-Pro-7-amido-4-trifluoromethylcoumarin as substrate after 1 hr by fluorescence assay | B | 7.72 | pIC50 | 19 | nM | IC50 | Bioorg Med Chem (2013) 21: 2795-2825 [PMID:23623674] |
| ChEMBL | Inhibition of DPP4 (unknown origin) | B | 7.72 | pIC50 | 19 | nM | IC50 | J Med Chem (2014) 57: 2197-2212 [PMID:24099035] |
| ChEMBL | Inhibition of DPP4 extracted from human Caco2 cells using H-Gly-Pro-AMC substrate after 10 mins by fluorescence assay | B | 7.72 | pIC50 | 19 | nM | IC50 | ACS Med Chem Lett (2015) 6: 602-606 [PMID:26005541] |
| ChEMBL | Inhibition of human DPP4 expressed in baculovirus system | B | 7.74 | pIC50 | 18 | nM | IC50 | Eur J Med Chem (2008) 43: 1603-1611 [PMID:18207285] |
| ChEMBL | Inhibition of DPP4 activity | B | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 3373-3377 [PMID:17434732] |
| ChEMBL | Inhibition of DPP4 | B | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 3384-3387 [PMID:17433672] |
| ChEMBL | Inhibition of DPP4 | B | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 3877-3879 [PMID:17502141] |
| ChEMBL | Inhibition of DPP4 | B | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 5934-5939 [PMID:17827003] |
| ChEMBL | In vitro inhibition of human DPP-4 activity | B | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 49-52 [PMID:17055272] |
| ChEMBL | Inhibition of DPP4 | B | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (2008) 51: 4359-4369 [PMID:18570365] |
| ChEMBL | Inhibition of DPP4 | B | 7.74 | pIC50 | 18 | nM | IC50 | Eur J Med Chem (2009) 44: 3318-3322 [PMID:19375196] |
| ChEMBL | Inhibition of DPP4 in presence of 50% human serum | B | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3596-3600 [PMID:20483603] |
| ChEMBL | Inhibition of DPP4 | B | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1880-1886 [PMID:21320777] |
| ChEMBL | Inhibition of DPP4 in human plasma using Gly-Pro-AMC as substrate by fluorimetric analysis | B | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem (2012) 20: 5864-5883 [PMID:22938786] |
| ChEMBL | Inhibition of human DPP-4 expressed in baculovirus expression system using H-Gly-Pro-AMC as substrate after 30 mins by fluorometric analysis | B | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 1918-1922 [PMID:24675378] |
| ChEMBL | Competitive reversible inhibition of DPP4 (unknown origin) | B | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (2014) 57: 3205-3212 [PMID:24660890] |
| ChEMBL | Inhibition of human DPP-4 using H-Gly-Pro-para-Nitroanilide as substrate incubated for 20 mins prior to substrate addition measured after 30 mins by spectrophotometry | B | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 3447-3451 [PMID:24948564] |
| ChEMBL | Inhibition of human recombinant DPP-4 using Gly-pro-p-nitroanilide as substrate assessed as formation of p-nitroaniline after 30 mins by colorimetric assay | B | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4428-4433 [PMID:26372650] |
| ChEMBL | Inhibition of DPP-4 (unknown origin) | B | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (2015) 58: 8315-8359 [PMID:26200936] |
| ChEMBL | Inhibition of DPP4 (unknown origin) using Gly-Pro-p-nitroanilide as substrate incubated for 1 hr | B | 7.77 | pIC50 | 17 | nM | IC50 | Eur J Med Chem (2016) 124: 103-116 [PMID:27560285] |
| ChEMBL | Inhibition of DPP4 (unknown origin) pre-incubated for 1 hr before Gly-Pro-pNA substrate addition and measured 2 hrs post substrate addition | B | 7.8 | pIC50 | 16 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 1872-1875 [PMID:25838146] |
| ChEMBL | Inhibition of human DPP4 | B | 7.92 | pIC50 | 12 | nM | IC50 | Medchemcomm (2014) 5: 1700-1707 |
| ChEMBL | Inhibition of human recombinant DPP4 (39 to 766) | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 731-736 [PMID:24439847] |
| ChEMBL | Inhibition of DPP4 (unknown origin) using Gly-Pro-p-nitroanilide as substrate incubated for 1 hr | B | 8.08 | pIC50 | 8.4 | nM | IC50 | Eur J Med Chem (2020) 188: 112017-112017 [PMID:31926470] |
| GtoPdb | - | - | 8.1 | pIC50 | 8.6 | nM | IC50 | Indian J Pharmacol (2010) 42: 229-33 [PMID:20927248] |
| ChEMBL | Inhibition of recombinant human DPP4 using Gly-Pro-AMC as substrate after 1 hr by fluorescence assay | B | 8.11 | pIC50 | 7.8 | nM | IC50 | Eur J Med Chem (2018) 151: 145-157 [PMID:29609120] |
| ChEMBL | Inhibition of recombinant human DPP4 using Gly-Pro-AMC as substrate incubated for 1 hr by fluorogenic assay | B | 8.11 | pIC50 | 7.8 | nM | IC50 | Bioorg Med Chem (2021) 29: 115861-115861 [PMID:33214038] |
| ChEMBL | Inhibition of DPP4 (unknown origin) | B | 8.15 | pIC50 | 7 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 731-736 [PMID:24439847] |
| ChEMBL | Inhibition of recombinant human DPP4 expressed in baculovirus infected Sf9 insect cells using Gly-Pro-AMC as substrate measured at 60 secs interval for 20 mins by fluorescence assay | B | 8.16 | pIC50 | 6.9 | nM | IC50 | Bioorg Med Chem (2019) 27: 644-654 [PMID:30642693] |
| ChEMBL | Inhibition of DPP4 (unknown origin) expressed in Sf9 cells using Gly-Pro-AMC substrate | B | 8.2 | pIC50 | 6.24 | nM | IC50 | J Med Chem (2016) 59: 6772-6790 [PMID:27396490] |
| ChEMBL | Inhibition of DPP4 in human plasma assessed as formation of 7-amino-4-methylcoumarin from glycyl-L-proline 4-methylcoumaryl-7-amide by fluorescence assay | B | 8.46 | pIC50 | 3.5 | nM | IC50 | Bioorg Med Chem (2011) 19: 5490-5499 [PMID:21865048] |
| dipeptidyl peptidase 4/Dipeptidyl peptidase IV in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3883] [GtoPdb: 1612] [UniProtKB: P28843] | ||||||||
| ChEMBL | Inhibition of ob/ob mouse plasma DPP4 | B | 7.34 | pIC50 | 46 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2313-2318 [PMID:28442252] |
| ChEMBL | Inhibition of DPP4 in C57BL/6 mouse serum pre-incubated for 5 mins followed by Gly-Pro-7-AMC substrate addition by fluorescence based assay | B | 7.83 | pIC50 | 14.7 | nM | IC50 | J Med Chem (2019) 62: 10919-10925 [PMID:31747282] |
| dipeptidyl peptidase 4/Dipeptidyl peptidase IV in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4653] [GtoPdb: 1612] [UniProtKB: P14740] | ||||||||
| ChEMBL | Inhibition of Wistar rat plasma DPP4 | B | 7.48 | pIC50 | 33 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2313-2318 [PMID:28442252] |
| dipeptidyl peptidase 9/Dipeptidyl peptidase IX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4793] [GtoPdb: 2357] [UniProtKB: Q86TI2] | ||||||||
| ChEMBL | Inhibition of DPP9 activity | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 3373-3377 [PMID:17434732] |
| ChEMBL | Inhibition of DPP9 | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 3384-3387 [PMID:17433672] |
| ChEMBL | Inhibition of DPP9 | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 3877-3879 [PMID:17502141] |
| ChEMBL | Inhibition of DPP9 | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 4154-4158 [PMID:18556199] |
| ChEMBL | Inhibition of DPP9 | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3596-3600 [PMID:20483603] |
| ChEMBL | Inhibition of human recombinant His-tagged DPP9 expressed in insect cells | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2010) 53: 6572-6583 [PMID:20718420] |
| ChEMBL | Inhibition of DPP9 | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1880-1886 [PMID:21320777] |
| ChEMBL | Inhibition of DPP9 | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2011) 54: 5737-5746 [PMID:21711053] |
| ChEMBL | Inhibition of DPP9 (unknown origin) | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2313-2318 [PMID:28442252] |
| ChEMBL | Inhibition of human recombinant DPP-9 using H-Gly-Pro-AMC as substrate after 10 mins by fluorescence assay | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 3731-3735 [PMID:30343953] |
| ChEMBL | Inhibition of human recombinant DPP9 using H-Gly-Pro-AMC substrate after 10 mins by fluorescence assay | B | 4.06 | pIC50 | 88000 | nM | IC50 | ACS Med Chem Lett (2015) 6: 602-606 [PMID:26005541] |
| ChEMBL | Inhibition of human recombinant DPP9 pre-incubated with compound for 15 mins before substrate addition by luminescence assay | B | 4.06 | pIC50 | 88000 | nM | IC50 | ACS Med Chem Lett (2014) 5: 921-926 [PMID:25147615] |
| ChEMBL | Inhibition of DPP9 (unknown origin) expressed in baculovirus expression system using Ala-Pro-AMC as substrate by continuous fluorometric assay | B | 4.17 | pIC50 | 67410 | nM | IC50 | Eur J Med Chem (2014) 86: 242-256 [PMID:25164763] |
| ChEMBL | Inhibition of DPP9 (unknown origin) | B | 4.21 | pIC50 | 62000 | nM | IC50 | Medchemcomm (2014) 5: 1700-1707 |
| ChEMBL | Inhibition of human recombinant DPP9 | B | 4.21 | pIC50 | 61900 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 731-736 [PMID:24439847] |
| ChEMBL | Inhibition of DPP9 | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem (2012) 20: 5864-5883 [PMID:22938786] |
| ChEMBL | Inhibition of recombinant his6-tagged DPP9 (unknown origin) using Ala-Pro-AMC as substrate by continuous fluorometric method | B | 5.51 | pIC50 | 3060 | nM | IC50 | Bioorg Med Chem (2014) 22: 6684-6693 [PMID:25457126] |
| dipeptidyl peptidase 8/Dipeptidyl peptidase VIII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4657] [GtoPdb: 2356] [UniProtKB: Q6V1X1] | ||||||||
| ChEMBL | Inhibition of DPP8 (unknown origin) | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2313-2318 [PMID:28442252] |
| ChEMBL | Inhibition of human recombinant His-tagged DPP8 expressed in insect cells | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2010) 53: 6572-6583 [PMID:20718420] |
| ChEMBL | Inhibition of DPP8 | B | 4.16 | pIC50 | 69000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1880-1886 [PMID:21320777] |
| ChEMBL | Inhibition of DPP8 (unknown origin) expressed in baculovirus expression system using Ala-Pro-AMC as substrate by continuous fluorometric assay | B | 4.17 | pIC50 | 67720 | nM | IC50 | Eur J Med Chem (2014) 86: 242-256 [PMID:25164763] |
| ChEMBL | Inhibition of human recombinant DPP-8 using H-Gly-Pro-AMC as substrate after 10 mins by fluorescence assay | B | 4.29 | pIC50 | 51000 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 3731-3735 [PMID:30343953] |
| ChEMBL | Inhibition of DPP8 | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 4154-4158 [PMID:18556199] |
| ChEMBL | Inhibition of DPP8 (unknown origin) | B | 4.3 | pIC50 | >50000 | nM | IC50 | Eur J Med Chem (2017) 139: 482-491 [PMID:28826083] |
| ChEMBL | Inhibition of DPP8 | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2011) 54: 5737-5746 [PMID:21711053] |
| ChEMBL | Inhibition of DPP8 | B | 4.32 | pIC50 | 48000 | nM | IC50 | Bioorg Med Chem (2012) 20: 5864-5883 [PMID:22938786] |
| ChEMBL | Inhibition of DPP8 | B | 4.32 | pIC50 | 48000 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 3384-3387 [PMID:17433672] |
| ChEMBL | Inhibition of DPP8 | B | 4.32 | pIC50 | 48000 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 3877-3879 [PMID:17502141] |
| ChEMBL | Inhibition of DPP8 activity | B | 4.32 | pIC50 | 48000 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 3373-3377 [PMID:17434732] |
| ChEMBL | Inhibition of recombinant his6-tagged DPP8 (unknown origin) expressed in baculovirus expression system using Ala-pro-AMC as substrate by fluorometric analysis | B | 4.47 | pIC50 | 33600 | nM | IC50 | Eur J Med Chem (2014) 75: 111-122 [PMID:24531224] |
| ChEMBL | Inhibition of human recombinant DPP8 | B | 4.48 | pIC50 | 32800 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 731-736 [PMID:24439847] |
| ChEMBL | Inhibition of human recombinant DPP8 using H-Gly-Pro-AMC substrate after 10 mins by fluorescence assay | B | 4.49 | pIC50 | 32000 | nM | IC50 | ACS Med Chem Lett (2015) 6: 602-606 [PMID:26005541] |
| ChEMBL | Inhibition of human recombinant DPP8 pre-incubated with compound for 15 mins before substrate addition by luminescence assay | B | 4.49 | pIC50 | 32000 | nM | IC50 | ACS Med Chem Lett (2014) 5: 921-926 [PMID:25147615] |
| ChEMBL | Inhibition of DPP8 | B | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3596-3600 [PMID:20483603] |
| ChEMBL | Inhibition of human DPP8 | B | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem (2009) 17: 2388-2399 [PMID:19261480] |
| ChEMBL | Inhibition of DPP8 | B | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 1908-1912 [PMID:19269819] |
| ChEMBL | Inhibition of DPP8 (unknown origin) | B | 4.72 | pIC50 | 19000 | nM | IC50 | Medchemcomm (2014) 5: 1700-1707 |
| ChEMBL | Inhibition of recombinant his6-tagged DPP8 (unknown origin) using Ala-Pro-AMC as substrate by continuous fluorometric method | B | 5.74 | pIC50 | 1820 | nM | IC50 | Bioorg Med Chem (2014) 22: 6684-6693 [PMID:25457126] |
| fibroblast activation protein alpha/Fibroblast activation protein alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4683] [GtoPdb: 2365] [UniProtKB: Q12884] | ||||||||
| ChEMBL | Inhibition of FAPalpha | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem (2012) 20: 5864-5883 [PMID:22938786] |
| ChEMBL | Inhibition of FAP | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 3877-3879 [PMID:17502141] |
| ChEMBL | Inhibition of FAP | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 3384-3387 [PMID:17433672] |
| ChEMBL | Inhibition of FAP | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3596-3600 [PMID:20483603] |
| ChEMBL | Inhibition of human recombinant FAP expressed in Hi5 insect cells | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2010) 53: 6572-6583 [PMID:20718420] |
| ChEMBL | Inhibition of FAP (unknown origin) | B | 4 | pIC50 | >100000 | nM | IC50 | Medchemcomm (2014) 5: 1700-1707 |
| ChEMBL | Inhibition of FAP in human U87MG cells using Suc-Gly-Pro-AMC as substrate by fluorescence based assay | B | 4.07 | pIC50 | 85340 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127253-127253 [PMID:32527554] |
| ChEMBL | Inhibition of FAP | B | 4.46 | pIC50 | >35000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1880-1886 [PMID:21320777] |
| ChEMBL | Inhibition of FAP (unknown origin) expressed in baculovirus expression system using Nle-Pro-AMC as substrate by continuous fluorometric assay | B | 4.52 | pIC50 | 30390 | nM | IC50 | Eur J Med Chem (2014) 86: 242-256 [PMID:25164763] |
| ChEMBL | Inhibition of human FAP | B | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem (2009) 17: 2388-2399 [PMID:19261480] |
| ChEMBL | Inhibition of recombinant his6-tagged FAP (unknown origin) using Nle-Pro-AMC as substrate by continuous fluorometric method | B | 5.23 | pIC50 | 5830 | nM | IC50 | Bioorg Med Chem (2014) 22: 6684-6693 [PMID:25457126] |
| Neutral endopeptidase/Neprilysin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1944] [GtoPdb: 1611] [UniProtKB: P08473] | ||||||||
| ChEMBL | Inhibition of NEP (unknown origin) | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2313-2318 [PMID:28442252] |
| prolyl endopeptidase/Prolyl endopeptidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3202] [GtoPdb: 2395] [UniProtKB: P48147] | ||||||||
| ChEMBL | Inhibition of human recombinant PREP expressed in Escherichia coli assessed as pNA release from Z-Gly-Pro-p-nitroanilide pre-incubated with enzyme for 15 mins prior to substrate addition by fluorescence technique | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 3412-3417 [PMID:22525314] |
| ChEMBL | Inhibition of PREP (unknown origin) | B | 4 | pIC50 | >100000 | nM | IC50 | Medchemcomm (2014) 5: 1700-1707 |
| ChEMBL | Inhibition of PPCE (unknown origin) | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2313-2318 [PMID:28442252] |
| fibroblast activation protein alpha/Seprase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5769] [GtoPdb: 2365] [UniProtKB: P97321] | ||||||||
| ChEMBL | Inhibition of mouse recombinant FAP expressed in HEK293 cells assessed as pNA release from Ala-Pro-p-nitroanilide pre-incubated with enzyme for 15 mins prior to substrate addition by fluorescence technique | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 3412-3417 [PMID:22525314] |
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]
