compound 2c [PMID: 24900538] | Ligand Activity Charts

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compound 2c [PMID: 24900538]
Ligand Activity Charts

compound 2c [PMID: 24900538] [Ligand Id: 8138] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2151321
ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73] There should be some charts here, you may need to enable JavaScript!
fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362] There should be some charts here, you may need to enable JavaScript!
protein tyrosine kinase 2/Focal adhesion kinase 1 in Human [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397] There should be some charts here, you may need to enable JavaScript!
K_v11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] 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!
mitogen-activated protein kinase kinase kinase 9/Mitogen-activated protein kinase kinase kinase 9 in Human [ChEMBL: CHEMBL2872] [GtoPdb: 2084] [UniProtKB: P80192] There should be some charts here, you may need to enable JavaScript!
muscle associated receptor tyrosine kinase/Muscle, skeletal receptor tyrosine protein kinase in Human [ChEMBL: CHEMBL5684] [GtoPdb: 1847] [UniProtKB: O15146] There should be some charts here, you may need to enable JavaScript!
neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629] There should be some charts here, you may need to enable JavaScript!
neurotrophic receptor tyrosine kinase 2/Neurotrophic tyrosine kinase receptor type 2 in Human [ChEMBL: CHEMBL4898] [GtoPdb: 1818] [UniProtKB: Q16620] There should be some charts here, you may need to enable JavaScript!
phosphorylase kinase catalytic subunit gamma 2/Phosphorylase kinase gamma subunit 2 in Human [ChEMBL: CHEMBL2349] [GtoPdb: 2147] [UniProtKB: P15735] There should be some charts here, you may need to enable JavaScript!
salt inducible kinase 1/Serine/threonine-protein kinase SIK1 in Human [ChEMBL: CHEMBL6082] [GtoPdb: 2197] [UniProtKB: P57059] There should be some charts here, you may need to enable JavaScript!
WNK lysine deficient protein kinase 3/Serine/threonine-protein kinase WNK3 in Human [ChEMBL: CHEMBL6055] [GtoPdb: 2282] [UniProtKB: Q9BYP7] There should be some charts here, you may need to enable JavaScript!
testis specific serine kinase 2/Testis-specific serine/threonine-protein kinase 2 in Human [ChEMBL: CHEMBL6014] [GtoPdb: 2258] [UniProtKB: Q96PF2] 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!
Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187] There should be some charts here, you may need to enable JavaScript!
FGR proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FGR in Human [ChEMBL: CHEMBL4454] [GtoPdb: 2024] [UniProtKB: P09769] There should be some charts here, you may need to enable JavaScript!
IL2 inducible T cell kinase/Tyrosine-protein kinase ITK/TSK in Human [ChEMBL: CHEMBL2959] [GtoPdb: 2046] [UniProtKB: Q08881] There should be some charts here, you may need to enable JavaScript!
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] 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] There should be some charts here, you may need to enable JavaScript!
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] There should be some charts here, you may need to enable JavaScript!
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949] There should be some charts here, you may need to enable JavaScript!
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!
fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916] 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
ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
ChEMBL	Inhibition of ALK	B	7.47	pIC50	34.1	nM	IC50	ACS Med. Chem. Lett. (2012) 3: 705-709 [PMID:24900538]
fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
GtoPdb	-	-	8.06	pIC50	8.7	nM	IC50	ACS Med Chem Lett (2012) 3: 705-9 [PMID:24900538]
ChEMBL	Inhibition of FGFR1	B	8.06	pIC50	8.7	nM	IC50	ACS Med. Chem. Lett. (2012) 3: 705-709 [PMID:24900538]
protein tyrosine kinase 2/Focal adhesion kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397]
ChEMBL	Inhibition of FAK	B	7.76	pIC50	17.2	nM	IC50	ACS Med. Chem. Lett. (2012) 3: 705-709 [PMID:24900538]
K_v11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL	Inhibition of human ERG	B	4.49	pIC50	>32000	nM	IC50	ACS Med. Chem. Lett. (2012) 3: 705-709 [PMID:24900538]
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
ChEMBL	Inhibition of SAPK2a	B	7.87	pIC50	13.4	nM	IC50	ACS Med. Chem. Lett. (2012) 3: 705-709 [PMID:24900538]
mitogen-activated protein kinase kinase kinase 9/Mitogen-activated protein kinase kinase kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2872] [GtoPdb: 2084] [UniProtKB: P80192]
ChEMBL	Inhibition of MLK1	B	7.35	pIC50	44.3	nM	IC50	ACS Med. Chem. Lett. (2012) 3: 705-709 [PMID:24900538]
muscle associated receptor tyrosine kinase/Muscle, skeletal receptor tyrosine protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5684] [GtoPdb: 1847] [UniProtKB: O15146]
ChEMBL	Inhibition of MuSk	B	7	pIC50	<100	nM	IC50	ACS Med. Chem. Lett. (2012) 3: 705-709 [PMID:24900538]
neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
ChEMBL	Amplified Luminescent Proximity Assay: To measure JAK2 kinase activity, a commercially available purified enzyme may be used. The enzyme may be a C-terminal His6-tagged, recombinant, human JAK2, amino acids 808-end, (Genbank Accession number NM 004972) expressed by baculovirus in Sf21 cells (Upstate Biotechnology MA). After incubation of the kinase with a biotinylated substrate and adenosine triphosphate (ATP) for 60 minutes at room temperature, the kinase reaction may be stopped by the addition of 30 mM ethylenediaminetetraacetic acid (EDTA). The reaction may be performed in 384 well microtitre plates and the reaction products may be detected with the addition of streptavidin coated Donor Beads and phosphotyrosine-specific antibodies coated Acceptor Beads using the EnVision Multilabel Plate Reader after an overnight incubation at room temperature.	B	8.52	pIC50	3	nM	IC50	US-8486966-B2. 9-(pyrazol-3-yl)-9H-purine-2-amine and 3-(pyrazol-3-yl) -3H-imidazo[4,5-B] pyridin-5-amine derivatives and their use for the treatment of cancer (2013)
GtoPdb	-	-	8.85	pIC50	1.4	nM	IC50	ACS Med Chem Lett (2012) 3: 705-9 [PMID:24900538]
ChEMBL	Inhibition of TrkA	B	8.85	pIC50	1.4	nM	IC50	ACS Med. Chem. Lett. (2012) 3: 705-709 [PMID:24900538]
neurotrophic receptor tyrosine kinase 2/Neurotrophic tyrosine kinase receptor type 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4898] [GtoPdb: 1818] [UniProtKB: Q16620]
ChEMBL	Inhibition of TrkB	B	7	pIC50	<100	nM	IC50	ACS Med. Chem. Lett. (2012) 3: 705-709 [PMID:24900538]
phosphorylase kinase catalytic subunit gamma 2/Phosphorylase kinase gamma subunit 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2349] [GtoPdb: 2147] [UniProtKB: P15735]
GtoPdb	-	-	8.21	pIC50	6.1	nM	IC50	ACS Med Chem Lett (2012) 3: 705-9 [PMID:24900538]
ChEMBL	Inhibition of PhKg2	B	8.21	pIC50	6.1	nM	IC50	ACS Med. Chem. Lett. (2012) 3: 705-709 [PMID:24900538]
salt inducible kinase 1/Serine/threonine-protein kinase SIK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6082] [GtoPdb: 2197] [UniProtKB: P57059]
ChEMBL	Inhibition of SIK	B	8.26	pIC50	5.5	nM	IC50	ACS Med. Chem. Lett. (2012) 3: 705-709 [PMID:24900538]
GtoPdb	-	-	8.26	pIC50	5.5	nM	IC50	ACS Med Chem Lett (2012) 3: 705-9 [PMID:24900538]
WNK lysine deficient protein kinase 3/Serine/threonine-protein kinase WNK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6055] [GtoPdb: 2282] [UniProtKB: Q9BYP7]
GtoPdb	-	-	7	pIC50	99.8	nM	IC50	ACS Med Chem Lett (2012) 3: 705-9 [PMID:24900538]
ChEMBL	Inhibition of WNK3	B	7	pIC50	99.8	nM	IC50	ACS Med. Chem. Lett. (2012) 3: 705-709 [PMID:24900538]
testis specific serine kinase 2/Testis-specific serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6014] [GtoPdb: 2258] [UniProtKB: Q96PF2]
GtoPdb	-	-	7.51	pIC50	30.6	nM	IC50	ACS Med Chem Lett (2012) 3: 705-9 [PMID:24900538]
ChEMBL	Inhibition of TSSK2	B	7.51	pIC50	30.6	nM	IC50	ACS Med. Chem. Lett. (2012) 3: 705-709 [PMID:24900538]
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
GtoPdb	-	-	8.92	pIC50	1.2	nM	IC50	ACS Med Chem Lett (2012) 3: 705-9 [PMID:24900538]
ChEMBL	Inhibition of Abl	B	8.92	pIC50	1.2	nM	IC50	ACS Med. Chem. Lett. (2012) 3: 705-709 [PMID:24900538]
Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187]
ChEMBL	Inhibition of BTK	B	8.46	pIC50	3.5	nM	IC50	ACS Med. Chem. Lett. (2012) 3: 705-709 [PMID:24900538]
GtoPdb	-	-	8.46	pIC50	3.5	nM	IC50	ACS Med Chem Lett (2012) 3: 705-9 [PMID:24900538]
FGR proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FGR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4454] [GtoPdb: 2024] [UniProtKB: P09769]
ChEMBL	Inhibition of Fgr	B	8.66	pIC50	2.2	nM	IC50	ACS Med. Chem. Lett. (2012) 3: 705-709 [PMID:24900538]
GtoPdb	-	-	8.66	pIC50	2.2	nM	IC50	ACS Med Chem Lett (2012) 3: 705-9 [PMID:24900538]
IL2 inducible T cell kinase/Tyrosine-protein kinase ITK/TSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2959] [GtoPdb: 2046] [UniProtKB: Q08881]
ChEMBL	Inhibition of Itk	B	7.14	pIC50	72.2	nM	IC50	ACS Med. Chem. Lett. (2012) 3: 705-709 [PMID:24900538]
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
ChEMBL	Inhibition of JAK2	B	7.17	pIC50	68.3	nM	IC50	ACS Med. Chem. Lett. (2012) 3: 705-709 [PMID:24900538]
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	7	pIC50	<100	nM	IC50	ACS Med. Chem. Lett. (2012) 3: 705-709 [PMID:24900538]
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL	Inhibition of Flt3	B	8.68	pIC50	2.1	nM	IC50	ACS Med. Chem. Lett. (2012) 3: 705-709 [PMID:24900538]
GtoPdb	-	-	8.68	pIC50	2.1	nM	IC50	ACS Med Chem Lett (2012) 3: 705-9 [PMID:24900538]
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
ChEMBL	Inhibition of Ret	B	7	pIC50	<100	nM	IC50	ACS Med. Chem. Lett. (2012) 3: 705-709 [PMID:24900538]
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
ChEMBL	Inhibition of cSrc	B	7.74	pIC50	18.2	nM	IC50	ACS Med. Chem. Lett. (2012) 3: 705-709 [PMID:24900538]
fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916]
ChEMBL	Inhibition of FLT4	B	7.19	pIC50	64	nM	IC50	ACS Med. Chem. Lett. (2012) 3: 705-709 [PMID:24900538]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]