sitagliptin [Ligand Id: 6286] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1422 (Januvia, LEZ763, LEZ-763, MK-0431, Sitagliptin)
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  • Dipeptidyl-peptidase 7/Dipeptidyl peptidase II in Human [ChEMBL: CHEMBL3976] [GtoPdb: 1605] [UniProtKB: Q9UHL4]
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  • Dipeptidyl peptidase IV in Porphyromonas gingivalis [ChEMBL: CHEMBL4295559] [UniProtKB: O31048]
  • 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]
  • dipeptidyl peptidase 4/Dipeptidyl peptidase IV in Rat [ChEMBL: CHEMBL4653] [GtoPdb: 1612] [UniProtKB: P14740]
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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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  • fibroblast activation protein alpha/Seprase in Mouse [ChEMBL: CHEMBL5769] [GtoPdb: 2365] [UniProtKB: P97321]
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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]