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 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]
