sitagliptin [Ligand Id: 6286] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL1422 (Januvia, LEZ-763, LEZ763, MK-0431, Sitagliptin, Sitagliptina, Sitagliptine) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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] |
| carbonic anhydrase 1/Carbonic anhydrase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL261] [GtoPdb: 2597] [UniProtKB: P00915] | ||||||||
| ChEMBL | Inhibition of human recombinant CA1 assessed as inhibition constant pre-incubated for 15 mins measured by phenol red dye based stopped flow CO2 hydration assay | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2022) 65: 13946-13966 [PMID:36201615] |
| carbonic anhydrase 2/Carbonic anhydrase II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918] | ||||||||
| ChEMBL | Inhibition of human recombinant CA2 assessed as inhibition constant pre-incubated for 15 mins measured by phenol red dye based stopped flow CO2 hydration assay | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2022) 65: 13946-13966 [PMID:36201615] |
| carbonic anhydrase 4/Carbonic anhydrase IV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3729] [GtoPdb: 2599] [UniProtKB: P22748] | ||||||||
| ChEMBL | Inhibition of human recombinant CA4 assessed as inhibition constant pre-incubated for 15 mins measured by phenol red dye based stopped flow CO2 hydration assay | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2022) 65: 13946-13966 [PMID:36201615] |
| carbonic anhydrase 9/Carbonic anhydrase IX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3594] [GtoPdb: 3055] [UniProtKB: Q16790] | ||||||||
| ChEMBL | Inhibition of human recombinant CA9 assessed as inhibition constant pre-incubated for 15 mins measured by phenol red dye based stopped flow CO2 hydration assay | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2022) 65: 13946-13966 [PMID:36201615] |
| carbonic anhydrase 5A/Carbonic anhydrase VA in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4789] [GtoPdb: 3093] [UniProtKB: P35218] | ||||||||
| ChEMBL | Inhibition of human recombinant CA5A assessed as inhibition constant pre-incubated for 15 mins measured by phenol red dye based stopped flow CO2 hydration assay | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2022) 65: 13946-13966 [PMID:36201615] |
| Carbonic anhydrase VB in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3969] [UniProtKB: Q9Y2D0] | ||||||||
| ChEMBL | Inhibition of human recombinant CA5B assessed as inhibition constant pre-incubated for 15 mins measured by phenol red dye based stopped flow CO2 hydration assay | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2022) 65: 13946-13966 [PMID:36201615] |
| 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 | Binding affinity to human DPP-4 using gly-pro-pNA as substrate assessed as inhibition constant | B | 7.74 | pKi | 18 | nM | Ki | J Med Chem (2023) 66: 11593-11631 [PMID:37647598] |
| ChEMBL | Inhibition of human recombinant DPP-4 using Gly-Pro-7-amido-4-methylcoumarin as substrate | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (2023) 66: 11593-11631 [PMID:37647598] |
| 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 DPP4 | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2011) 54: 5737-5746 [PMID:21711053] |
| 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 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 DPP-4 (unknown origin) | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem (2021) 46: 116354-116354 [PMID:34428715] |
| 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 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 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 plasma DPP4 | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2313-2318 [PMID:28442252] |
| 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 human recombinant DPP-4 expressed in human Caco-2 cells using H-Ala-Pro-7-amido-4-trifluoromethylcoumarin as substrate measured after 1 hrs by fluorescence based assay | B | 7.72 | pIC50 | 19 | nM | IC50 | J Med Chem (2023) 66: 11593-11631 [PMID:37647598] |
| 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 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 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 DPP4 | B | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (2008) 51: 4359-4369 [PMID:18570365] |
| 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 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 DPP4 | B | 7.74 | pIC50 | 18 | nM | IC50 | Eur J Med Chem (2009) 44: 3318-3322 [PMID:19375196] |
| 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 | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (2023) 66: 11593-11631 [PMID:37647598] |
| 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 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 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 | B | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 5934-5939 [PMID:17827003] |
| 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: 3384-3387 [PMID:17433672] |
| 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 DPP-4 (unknown origin) incubated for 30 mins in presence of substrate by fluorescence based analysis | B | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (2023) 66: 991-1010 [PMID:36584305] |
| ChEMBL | Inhibition of DPP-4 (unknown origin) | B | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (2023) 66: 11593-11631 [PMID:37647598] |
| 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 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 (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 recombinant DPP-4 in Caco-2 cells using GP-AMC as substrate by fluorescence based assay | B | 7.8 | pIC50 | 16 | nM | IC50 | J Med Chem (2023) 66: 11593-11631 [PMID:37647598] |
| 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 human recombinant DPP4 using H-Gly-Pro-AMC as substrate incubated for 30 mins by fluorescence based microplate reader assay | B | 8.06 | pIC50 | 8.8 | nM | IC50 | J Med Chem (2022) 65: 13946-13966 [PMID:36201615] |
| 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] |
| ChEMBL | Inhibition of human DPP-4 expressed in human Caco-2 cells using H-Gly-Pro-AMC as substrate measured for 30 mins by microplate reader analysis | B | 9.06 | pIC50 | 0.87 | nM | IC50 | Bioorg Med Chem (2021) 46: 116354-116354 [PMID:34428715] |
| 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 mouse DPP-4 using Gly-Pro-AMC as substrate measured after 5 mins by CF assay | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2023) 66: 11593-11631 [PMID:37647598] |
| 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] |
| ChEMBL | Inhibition of human recombinant PEP expressed in baculovirus expression system using Ala-Pro-7-amido-4-trifluoromethylcoumarin as substrate by fluorescence based assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2023) 66: 11593-11631 [PMID:37647598] |
| 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 34:
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]
