ChEMBL ligand: CHEMBL406845 (AG-1879)
casein kinase 1 delta/Casein kinase I delta in Human [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730] There should be some charts here, you may need to enable JavaScript!
EPH receptor B2/Ephrin type-B receptor 2 in Human [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323] There should be some charts here, you may need to enable JavaScript!
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] There should be some charts here, you may need to enable JavaScript!
receptor interacting serine/threonine kinase 2/Serine/threonine-protein kinase RIPK2 in Human [ChEMBL: CHEMBL5014] [GtoPdb: 2190] [UniProtKB: O43353] There should be some charts here, you may need to enable JavaScript!
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519] There should be some charts here, you may need to enable JavaScript!
FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241] There should be some charts here, you may need to enable JavaScript!
HCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase HCK in Human [ChEMBL: CHEMBL3234] [GtoPdb: 2032] [UniProtKB: P08631] There should be some charts here, you may need to enable JavaScript!
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] There should be some charts here, you may need to enable JavaScript!
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] 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
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]
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
ChEMBL	Inhibition of p38 alpha (unknown origin) using Ser/Thr 15 as substrate incubated for 1 hr in presence of ATP by Z'-Lyte assay	B	5.37	pIC50	4230	nM	IC50	Eur J Med Chem (2021) 215: 113277-113277 [PMID:33601311]
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]
ChEMBL	Inhibition of FYN (unknown origin)	B	8.3	pIC50	5	nM	IC50	RSC Med Chem (2022) 13: 1008-1028 [PMID:36324498]
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]
ChEMBL	Inhibition of LCK (unknown origin)	B	8.4	pIC50	4	nM	IC50	RSC Med Chem (2022) 13: 1008-1028 [PMID:36324498]
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	Binding affinity to chicken 6-His tagged c-Src expressed in Escherichia coli Bl21 (DE3) assessed as dissociation constant	B	6.53	pKd	296	nM	Kd	Eur J Med Chem (2021) 216: 113318-113318 [PMID:33730624]
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 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]