1G244 [Ligand Id: 8551] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1814633 |
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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 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 | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2011) 54: 5737-5746 [PMID:21711053] |
| ChEMBL | Inhibition of DPP2 in human seminal plasma using Lys-Ala-p-nitroanilide as substrate preincubated for 15 mins followed by substrate addition measured for 10 mins by spectrofluorimetry | B | 4.3 | pIC50 | >50000 | nM | IC50 | Medchemcomm (2016) 7: 433-438 |
| dipeptidyl peptidase 4/Dipeptidyl peptidase IV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL284] [GtoPdb: 1612] [UniProtKB: P27487] | ||||||||
| ChEMBL | Inhibition of DPP4 | B | 4 | pIC50 | >100000 | 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 | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2011) 54: 5737-5746 [PMID:21711053] |
| ChEMBL | Inhibition of DPP4 in human seminal plasma using Gly-Pro-p-nitroanilide as substrate preincubated for 15 mins followed by substrate addition measured for 10 mins by spectrofluorimetry | B | 4.3 | pIC50 | >50000 | nM | IC50 | Medchemcomm (2016) 7: 433-438 |
| dipeptidyl peptidase 9/Dipeptidyl peptidase IX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4793] [GtoPdb: 2357] [UniProtKB: Q86TI2] | ||||||||
| ChEMBL | Inhibition of DPP9 | B | 7.28 | pIC50 | 53 | nM | IC50 | J Med Chem (2011) 54: 5737-5746 [PMID:21711053] |
| GtoPdb | - | - | 7.28 | pIC50 | 53 | nM | IC50 | Biochem Pharmacol (2009) 78: 203-10 [PMID:19439267] |
| dipeptidyl peptidase 8/Dipeptidyl peptidase VIII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4657] [GtoPdb: 2356] [UniProtKB: Q6V1X1] | ||||||||
| GtoPdb | - | - | 7.85 | pIC50 | 14 | nM | IC50 | Biochem Pharmacol (2009) 78: 203-10 [PMID:19439267] |
| ChEMBL | Inhibition of DPP8 | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2011) 54: 5737-5746 [PMID:21711053] |
| ChEMBL | Inhibition of recombinant human DPP8 assessed as pNA release from Ala-Pro- p-nitroanilide substrate pre-incubated with enzyme for 15 min prior to substrate addition by fluorescence technique | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (2011) 54: 5737-5746 [PMID:21711053] |
| ChEMBL | Inhibition of full length human DPP8 expressed in baculovirus infected sf9 cells using Ala-Pro-p-nitroanilide as substrate preincubated for 15 mins followed by substrate addition measured for 10 mins by spectrofluorimetry | B | 7.92 | pIC50 | 12 | nM | IC50 | Medchemcomm (2016) 7: 433-438 |
| fibroblast activation protein alpha/Seprase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5769] [GtoPdb: 2365] [UniProtKB: P97321] | ||||||||
| ChEMBL | Inhibition of BALB/c mouse 5'-His6-tagged 3'-FLAG-tagged FAP fused with ECD expressed in HEK293 cells using Ala-Pro-p-nitroanilide as substrate preincubated for 15 mins followed by substrate addition measured for 10 mins by spectrofluorimetry | B | 4 | pIC50 | >100000 | nM | IC50 | Medchemcomm (2016) 7: 433-438 |
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]
