PP2 [Ligand Id: 9404] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL406845 (AG-1879)
  • casein kinase 1 delta/Casein kinase I delta in Human [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730]
  • This target only has 0 pki data point
  • 0
1 CHEMBL406845_lig_chart_1 Casein kinase I delta Human
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  • EPH receptor B2/Ephrin type-B receptor 2 in Human [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323]
  • This target only has 0 pki data point
  • 0
2 CHEMBL406845_lig_chart_2 Ephrin type-B receptor 2 Human
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
  • This target only has 1 pki data point
  • 5
3 CHEMBL406845_lig_chart_3 Epidermal growth factor receptor erbB1 Human
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  • receptor interacting serine/threonine kinase 2/Serine/threonine-protein kinase RIPK2 in Human [ChEMBL: CHEMBL5014] [GtoPdb: 2190] [UniProtKB: O43353]
  • This target only has 0 pki data point
  • 0
4 CHEMBL406845_lig_chart_4 Serine/threonine-protein kinase RIPK2 Human
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  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
  • This target only has 1 pki data point
  • 6.3
5 CHEMBL406845_lig_chart_5 Tyrosine-protein kinase ABL Human
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  • FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
  • This target only has 0 pki data point
  • 0
6 CHEMBL406845_lig_chart_6 Tyrosine-protein kinase FYN Human
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  • HCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase HCK in Human [ChEMBL: CHEMBL3234] [GtoPdb: 2032] [UniProtKB: P08631]
  • This target only has 0 pki data point
  • 0
7 CHEMBL406845_lig_chart_7 Tyrosine-protein kinase HCK Human
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  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Mouse [ChEMBL: CHEMBL2480] [GtoPdb: 2053] [UniProtKB: P06240]
  • This target only has 1 pki data point
  • 0
8 CHEMBL406845_lig_chart_8 Tyrosine-protein kinase LCK HumanMouse
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  • Tyrosine-protein kinase SRC in Chicken [ChEMBL: CHEMBL3655] [UniProtKB: P00523]
  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
  • 6.3
9 CHEMBL406845_lig_chart_9 Tyrosine-protein kinase SRC ChickenHuman
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
casein kinase 1 delta/Casein kinase I delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730]
ChEMBL Inhibition of CK1delta in the presence of 20uM ATP B 7.39 pIC50 41 nM IC50 Biochem. J. (2007) 408: 297-315 [PMID:17850214]
EPH receptor B2/Ephrin type-B receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323]
ChEMBL Equilibrium binding constant for EPH receptor B2 B 4.44 pKd 36500 nM Kd J. Med. Chem. (2005) 48: 3221-3230 [PMID:15857128]
ChEMBL Inhibition of EPH receptor B2 using ELISA B 4.28 pIC50 52000 nM IC50 J. Med. Chem. (2005) 48: 3221-3230 [PMID:15857128]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibition of EGFR B 5 pKi >10000 nM Ki ACS Med. Chem. Lett. (2012) 3: 383-386 [PMID:24900482]
ChEMBL Inhibition of EGFR B 6.32 pIC50 480 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
receptor interacting serine/threonine kinase 2/Serine/threonine-protein kinase RIPK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5014] [GtoPdb: 2190] [UniProtKB: O43353]
ChEMBL Inhibition of RIP2 in the presence of 100uM ATP B 7.72 pIC50 19 nM IC50 Biochem. J. (2007) 408: 297-315 [PMID:17850214]
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
ChEMBL Binding affinity to human recombinant Abl by cell free assay B 6.3 pKi 500 nM Ki J. Med. Chem. (2008) 51: 1252-1259 [PMID:18257513]
FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
ChEMBL Inhibition of FYN (unknown origin) by cell culture based assay B 8 pIC50 10 nM IC50 Eur J Med Chem (2017) 142: 229-243 [PMID:28814374]
GtoPdb - - 8.3 pIC50 5 nM IC50 J Biol Chem (1996) 271: 695-701 [PMID:8557675]
HCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase HCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3234] [GtoPdb: 2032] [UniProtKB: P08631]
ChEMBL Inhibition of Hck B 8.3 pIC50 5 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
ChEMBL Inhibition of LCK B 9.1 pKi 0.79 nM Ki ACS Med. Chem. Lett. (2012) 3: 383-386 [PMID:24900482]
ChEMBL Inhibition of p56 Lck tyrosine kinase in Jurkat cells where p56lck autophosphorylation is inhibited. B 8.4 pIC50 4 nM IC50 Bioorg. Med. Chem. Lett. (1997) 7: 417-420
ChEMBL Inhibition of p56lck autophosphorylation B 8.4 pIC50 4 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
GtoPdb - - 8.4 pIC50 4 nM IC50 J Biol Chem (1996) 271: 695-701 [PMID:8557675]
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2480] [GtoPdb: 2053] [UniProtKB: P06240]
ChEMBL Inhibition of Lck in the presence of 50uM ATP B 7.51 pIC50 31 nM IC50 Biochem. J. (2007) 408: 297-315 [PMID:17850214]
Tyrosine-protein kinase SRC in Chicken (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3655] [UniProtKB: P00523]
ChEMBL Inhibition of Src in the presence of 50uM ATP B 7.44 pIC50 36 nM IC50 Biochem. J. (2007) 408: 297-315 [PMID:17850214]
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
ChEMBL Inhibitory activity against Src in cell free assay B 6.3 pKi 500 nM Ki J. Med. Chem. (2006) 49: 1549-1561 [PMID:16509573]
ChEMBL Inhibition of human recombinant Src B 6.3 pKi 500 nM Ki J. Med. Chem. (2007) 50: 5579-5588 [PMID:17929792]
ChEMBL Inhibition of GST-tagged c-Src preincubated for 30 mins measured after 60 mins B 5.55 pIC50 2800 nM IC50 Bioorg. Med. Chem. (2012) 20: 6821-6830 [PMID:23098606]
ChEMBL Inhibition of c-Src after 60 mins B 5.55 pIC50 2800 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 449-452 [PMID:21084189]
ChEMBL Inhibition of GST-fussed c-SRC after 30 mins B 5.55 pIC50 2800 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 1342-1346 [PMID:21300544]
ChEMBL Inhibition of His6-tagged c-Src kinase domain using AEEEIYGEFEAKKKK as substrate pre-incubated for 10 mins before substrate addition measured after 30 mins by Transcreener ADP2 FI Assay B 6.3 pIC50 500 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 410-414 [PMID:22119472]
ChEMBL Inhibition of 6xHis-tagged Src catalytic domain (unknown origin) expressed in Escherichia coli using AEEEIYGEFEAKKKK as substrate incubated for 10 mins prior to substrate addition measured after 30 mins by fluorescence intensity assay B 6.3 pIC50 500 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 3230-3234 [PMID:23602444]
ChEMBL Inhibition cSRC B 7.3 pIC50 50 nM IC50 Bioorg. Med. Chem. (2010) 18: 4615-4624 [PMID:20570525]
ChEMBL Inhibition of Src (unknown origin) using Src-family kinase bisamide rhodamine 110 peptide substrate after 1 hr by fluorescence assay B 9.3 pIC50 0.5 nM IC50 Eur J Med Chem (2018) 157: 503-526 [PMID:30114661]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]