ChEMBL ligand: CHEMBL3125890
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!
cyclin dependent kinase 2/CDK2/Cyclin A2 in Human [ChEMBL: CHEMBL3038469] [GtoPdb: 1973] [UniProtKB: P20248, P24941] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase 8/c-Jun N-terminal kinase 1 in Human [ChEMBL: CHEMBL2276] [GtoPdb: 1496] [UniProtKB: P45983] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493, P14635] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase kinase 1/Dual specificity mitogen-activated protein kinase kinase 1 in Human [ChEMBL: CHEMBL3587] [GtoPdb: 2062] [UniProtKB: Q02750] 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!
fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607] There should be some charts here, you may need to enable JavaScript!
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841] There should be some charts here, you may need to enable JavaScript!
Heat shock factor protein 1 in Human [ChEMBL: CHEMBL5869] [UniProtKB: Q00613] There should be some charts here, you may need to enable JavaScript!
MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581] There should be some charts here, you may need to enable JavaScript!
inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa B kinase beta subunit in Human [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920] There should be some charts here, you may need to enable JavaScript!
Insulin receptor in Human [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase 3/MAP kinase ERK1 in Human [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361] 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 1/Mitogen-activated protein kinase kinase kinase 1 in Human [ChEMBL: CHEMBL3956] [GtoPdb: 2069] [UniProtKB: Q13233] There should be some charts here, you may need to enable JavaScript!
Pirin in Human [ChEMBL: CHEMBL2010627] [UniProtKB: O00625] There should be some charts here, you may need to enable JavaScript!
platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619] There should be some charts here, you may need to enable JavaScript!
Platelet-derived growth factor subunit A in Human [ChEMBL: CHEMBL3137294] [UniProtKB: P04085] There should be some charts here, you may need to enable JavaScript!
protein kinase C theta/Protein kinase C theta in Human [ChEMBL: CHEMBL3920] [GtoPdb: 1488] [UniProtKB: Q04759] There should be some charts here, you may need to enable JavaScript!
receptor interacting serine/threonine kinase 1/Receptor-interacting serine/threonine-protein kinase 1 in Human [ChEMBL: CHEMBL5464] [GtoPdb: 2189] [UniProtKB: Q13546] There should be some charts here, you may need to enable JavaScript!
receptor interacting serine/threonine kinase 3/Receptor-interacting serine/threonine-protein kinase 3 in Human [ChEMBL: CHEMBL1795199] [GtoPdb: 2191] [UniProtKB: Q9Y572] There should be some charts here, you may need to enable JavaScript!
erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626] There should be some charts here, you may need to enable JavaScript!
aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4] There should be some charts here, you may need to enable JavaScript!
B-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase B-raf in Human [ChEMBL: CHEMBL5145] [GtoPdb: 1943] [UniProtKB: P15056] There should be some charts here, you may need to enable JavaScript!
checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757] There should be some charts here, you may need to enable JavaScript!
Raf-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase RAF in Human [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049] There should be some charts here, you may need to enable JavaScript!
KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721] 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!
TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763] There should be some charts here, you may need to enable JavaScript!
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] 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 (unknown origin) using CK1tide as substrate after 20 mins	B	5	pIC50	>10000	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
cyclin dependent kinase 2/CDK2/Cyclin A2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038469] [GtoPdb: 1973] [UniProtKB: P20248, P24941]
ChEMBL	Inhibition of CDK2/CycA (unknown origin) using histone H1 as substrate after 20 mins	B	6.24	pIC50	580	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
mitogen-activated protein kinase 8/c-Jun N-terminal kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2276] [GtoPdb: 1496] [UniProtKB: P45983]
ChEMBL	Inhibition of C-terminal FLAG-tagged JNK1 (unknown origin) expressed in baculovirus system using c-jun as substrate after 60 mins	B	5	pIC50	>10000	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493, P14635]
ChEMBL	Inhibition of CDK1/CycB (unknown origin) using histone H1 as substrate after 20 mins	B	6.1	pIC50	790	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
mitogen-activated protein kinase kinase 1/Dual specificity mitogen-activated protein kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3587] [GtoPdb: 2062] [UniProtKB: Q02750]
ChEMBL	Inhibition of N-terminal GST-tagged MEK1 (unknown origin) expressed in 293 cells using GST-ERK1(K71A) as substrate after 20 mins	B	5.43	pIC50	3700	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
ChEMBL	In Vitro Inhibition Assay: MEK phosphorylation inhibition activity.	B	6.52	pIC50	<300	nM	IC50	US-8497274-B2. Heterocyclic compound and use thereof (2013)
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL	Inhibition of N-terminal peptide (DYKDDDD)-tagged EGFR (unknown origin) expressed in baculovirus system using biotinylated poly-Glu-Tyr (4:1) as substrate preincubated for 5 mins measured after 12 hrs by scintillation counting	B	5	pIC50	>10000	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607]
GtoPdb	Biochemical enzyme inhibition assay.	-	6.55	pIC50	280	nM	IC50	J Med Chem (2013) 56: 6478-94 [PMID:23906342]
ChEMBL	Inhibition of FGFR3 (unknown origin) using biotinylated poly-Glu-Tyr (4:1) as substrate preincubated for 5 mins measured after 12 hrs	B	6.55	pIC50	280	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
ChEMBL	Inhibition of C-terminal FLAG-tagged GSK3beta (unknown origin) expressed in baculovirus system after 30 mins	B	6.3	pIC50	500	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
Heat shock factor protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5869] [UniProtKB: Q00613]
ChEMBL	Inhibition of 17-AAG-induced HSF1 pathway in human SKOV3 cells assessed as reduction in HSP72 induction preincubated for 1 hr followed by 17-AAG addition measured after 18 hrs by ELISA	B	5	pIC50	>10000	nM	IC50	J Med Chem (2017) 60: 180-201 [PMID:28004573]
ChEMBL	Inhibition of 17-AAG-induced HSF1 pathway in human SKOV3 cells assessed as reduction in HSP72 induction preincubated for 1 hr followed by 17-AAG addition measured after 18 hrs by ELISA	B	5	pIC50	>10000	nM	IC50	J Med Chem (2017) 60: 180-201 [PMID:28004573]
MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
ChEMBL	Inhibition of c-Met receptor (unknown origin) using biotinylated poly-Glu-Tyr (4:1) as substrate preincubated for 5 mins measured after 12 hrs	B	5	pIC50	>10000	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa B kinase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920]
ChEMBL	Inhibition of C-terminal FLAG-tagged IKK beta (unknown origin) expressed in baculovirus system using IkappaBalpha as substrate after 40 mins	B	5.43	pIC50	3700	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213]
ChEMBL	Inhibition of Insulin receptor (unknown origin) using biotinylated poly-Glu-Tyr (4:1) as substrate preincubated for 5 mins measured after 12 hrs	B	5	pIC50	>10000	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
mitogen-activated protein kinase 3/MAP kinase ERK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361]
ChEMBL	Inhibition of C-terminal FLAG-tagged ERK1 expressed in baculovirus system (unknown origin) using MBP as substrate after 60 mins	B	5	pIC50	>10000	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
ChEMBL	Inhibition of C-terminal FLAG-tagged p38 alpha (unknown origin) expressed in baculovirus system using MBP as substrate after 60 mins	B	6.22	pIC50	600	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
mitogen-activated protein kinase kinase kinase 1/Mitogen-activated protein kinase kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3956] [GtoPdb: 2069] [UniProtKB: Q13233]
ChEMBL	Inhibition of C-terminal FLAG-tagged MEKK1 (unknown origin) expressed in baculovirus system using MBP as substrate after 60 mins	B	5	pIC50	>10000	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
Pirin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2010627] [UniProtKB: O00625]
ChEMBL	Displacement of 6-amino-9-(2-((4-((2-((6-((5-(2,3-dihydrobenzo[b][1,4]dioxine-6-carboxamido)-2-methylphenyl)carbamoyl)quinolin-2-yl)oxy)ethyl)amino)-4-oxobutyl)(methyl)carbamoyl)phenyl)-3-imino-3H-xanthene-4,5-disulfonic acid from pirin (unknown origin) by fluorescence polarization assay	B	5	pIC50	>10000	nM	IC50	ACS Med Chem Lett (2018) 9: 1199-1204 [PMID:30613326]
platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619]
GtoPdb	Biochemical enzyme inhibition assay.	-	6.92	pIC50	120	nM	IC50	J Med Chem (2013) 56: 6478-94 [PMID:23906342]
ChEMBL	Inhibition of PDGFR beta (unknown origin) using biotinylated poly-Glu-Tyr (4:1) as substrate preincubated for 5 mins measured after 12 hrs	B	6.92	pIC50	120	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
Platelet-derived growth factor subunit A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3137294] [UniProtKB: P04085]
ChEMBL	Inhibition of PDGFR alpha (unknown origin) using biotinylated poly-Glu-Tyr (4:1) as substrate preincubated for 5 mins measured after 12 hrs	B	6.21	pIC50	610	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
protein kinase C theta/Protein kinase C theta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3920] [GtoPdb: 1488] [UniProtKB: Q04759]
ChEMBL	Inhibition of C-terminal FLAG-tagged PKC-theta (unknown origin) expressed in Escherichia coli using MBP as substrate after 60 mins	B	5	pIC50	>10000	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
receptor interacting serine/threonine kinase 1/Receptor-interacting serine/threonine-protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5464] [GtoPdb: 2189] [UniProtKB: Q13546]
ChEMBL	Inhibition of human wild type RIPK1 (M1 to K305) expressed in bacterial system by kinomescan assay	B	6.32	pKd	480	nM	Kd	Bioorg Med Chem Lett (2021) 43: 128084-128084 [PMID:33964444]
GtoPdb	Binding constant determined by KINOMEscan assay.	-	6.32	pKd	480	nM	Kd	Br J Pharmacol (2019) 176: 2095-2108 [PMID:30825190]
receptor interacting serine/threonine kinase 3/Receptor-interacting serine/threonine-protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795199] [GtoPdb: 2191] [UniProtKB: Q9Y572]
ChEMBL	Binding affinity to wild-type human partial length RIPK3 (M1 to Q307 residues) expressed in bacterial expression system after 1 hr by quantitative PCR based KINOMEscan assay	B	6.98	pKd	105	nM	Kd	J Med Chem (2019) 62: 6665-6681 [PMID:31095385]
ChEMBL	Inhibition of human wild type RIPK3 (M1 to Q307) expressed in bacterial system by kinomescan assay	B	6.98	pKd	105	nM	Kd	Bioorg Med Chem Lett (2021) 43: 128084-128084 [PMID:33964444]
GtoPdb	Binding constant determined by KINOMEscan assay.	-	6.98	pKd	105	nM	Kd	Br J Pharmacol (2019) 176: 2095-2108 [PMID:30825190]
erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626]
ChEMBL	Inhibition of N-terminal peptide (DYKDDDD)-tagged HER2 (unknown origin) expressed in baculovirus system using biotinylated poly-Glu-Tyr (4:1) as substrate preincubated for 5 mins measured after 12 hrs by scintillation counting	B	5	pIC50	>10000	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
GtoPdb	Biochemical enzyme inhibition assay.	-	7.18	pIC50	66	nM	IC50	J Med Chem (2013) 56: 6478-94 [PMID:23906342]
ChEMBL	Inhibition of N-terminal His-6-tagged Aurora kinase B (unknown origin) expressed in baculovirus system after 60 mins	B	7.18	pIC50	66	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
B-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase B-raf in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5145] [GtoPdb: 1943] [UniProtKB: P15056]
GtoPdb	Dissociation constant determined using Surface Plasmon Resonance.	-	8.8	pKd	1.6	nM	Kd	J Med Chem (2013) 56: 6478-94 [PMID:23906342]
ChEMBL	Inhibition of recombinant wild type full length human GST-tagged B-Raf expressed in baculovirus expression system using Z'-LYTE Ser/Thr3 peptide as substrate incubated for 1 hr by FRET-based Z'-LYTE assay	B	7.11	pIC50	77	nM	IC50	Bioorg Med Chem Lett (2016) 26: 2760-2763 [PMID:27155899]
ChEMBL	Inhibition of BRAF V600E mutant in human HT-29 cells assessed as phosphorylation of MEK	B	7.12	pIC50	75	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
ChEMBL	Inhibition of BRAF V600E mutant (unknown origin) in presence of 1000 uM ATP by ELISA	B	7.24	pIC50	58	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
ChEMBL	Inhibition of BRAF V600E mutant in human A375 cells assessed as phosphorylation of ERK after 2 hrs by Western blotting analysis	B	7.8	pIC50	16	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
ChEMBL	Inhibition of recombinant human N-terminal GST-tagged B-Raf V600E mutant expressed in baculovirus expression system using Z'-LYTE Ser/Thr3 peptide as substrate incubated for 1 hr by FRET-based Z'-LYTE assay	B	7.82	pIC50	15	nM	IC50	Bioorg Med Chem Lett (2016) 26: 2760-2763 [PMID:27155899]
ChEMBL	Competitive inhibition of BRAF V600E mutant (unknown origin) in presence of 5 uM ATP by ELISA	B	7.82	pIC50	15	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
ChEMBL	Inhibition of BRAF V600E mutant in human A375 cells assessed as phosphorylation of MEK after 2 hrs by Western blotting analysis	B	7.92	pIC50	12	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
GtoPdb	Biochemical enzyme inhibition assay.	-	8.08	pIC50	8.3	nM	IC50	J Med Chem (2013) 56: 6478-94 [PMID:23906342]
ChEMBL	Inhibition of human full length wild type B-Raf	B	8.08	pIC50	8.3	nM	IC50	Eur J Med Chem (2020) 206: 112675-112675 [PMID:32798788]
ChEMBL	Inhibition of N-terminal FLAG-tagged wild type BRAF (unknown origin) expressed in baculovirus system using GST-MEK1(K96R) as substrate after 20 mins	B	8.08	pIC50	8.3	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
ChEMBL	Inhibition of recombinant human full length GST-tagged BRAF expressed in baculovirus expression system	B	8.1	pIC50	8	nM	IC50	ACS Med Chem Lett (2018) 9: 1199-1204 [PMID:30613326]
ChEMBL	Inhibition of N-terminal 6x-His-tagged BRAF V600E mutant (unknown origin) expressed in baculovirus infected Sf9 insect cells co-expressing mouse p50cdc37 using C-terminal His-tagged/N-terminal GST-tagged full length human MEK1 as substrate after 1 hr by ELISA	B	8.35	pIC50	4.48	nM	IC50	J Med Chem (2018) 61: 5034-5046 [PMID:29727562]
ChEMBL	Inhibition of BRAF V600E mutant (unknown origin) compound preincubated for 1 hr in presence of 1000 uM ATP	B	8.48	pIC50	3.3	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
ChEMBL	Inhibition of N-terminal 6x-His-tagged BRAF kinase domain (unknown origin) expressed in baculovirus infected Sf9 insect cells co-expressing mouse p50cdc37 using C-terminal His-tagged/N-terminal GST-tagged full length human MEK1 as substrate after 1 hr by ELISA	B	8.49	pIC50	3.23	nM	IC50	J Med Chem (2018) 61: 5034-5046 [PMID:29727562]
ChEMBL	Inhibition of N-terminal FLAG-tagged recombinant BRAF V600E mutant (unknown origin) expressed in baculovirus system preincubated for 10 mins before substrate addition measured after 20 mins by scintillation counting	B	8.62	pIC50	2.4	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
ChEMBL	Inhibition of B-Raf V600E mutant (unknown origin)	B	8.62	pIC50	2.4	nM	IC50	Eur J Med Chem (2020) 206: 112675-112675 [PMID:32798788]
ChEMBL	Inhibition of BRAF V600E mutant (unknown origin) compound preincubated for 1 hr in presence of 5 uM ATP	B	8.66	pIC50	2.2	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
ChEMBL	Inhibition of recombinant human GST-tagged BRAF V600E mutant expressed in baculovirus expression system	B	8.7	pIC50	2	nM	IC50	ACS Med Chem Lett (2018) 9: 1199-1204 [PMID:30613326]
checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757]
ChEMBL	Inhibition of CHK1 (unknown origin) using alpha-casein as substrate after 20 mins	B	5.85	pIC50	1400	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
Raf-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase RAF in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049]
GtoPdb	Dissociation constant determined by Surface Plasmon Resonance.	-	9.28	pKd	0.52	nM	Kd	J Med Chem (2013) 56: 6478-94 [PMID:23906342]
ChEMBL	Inhibition of CRAF (unknown origin) in presence of 1000 uM ATP by ELISA	B	7.21	pIC50	62	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
ChEMBL	Competitive inhibition of CRAF (unknown origin) in presence of 0.5 uM ATP by ELISA	B	8.09	pIC50	8.1	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
ChEMBL	Inhibition of CRAF (unknown origin) compound preincubated for 1 hr in presence of 1000 uM ATP	B	8.3	pIC50	5	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
ChEMBL	Inhibition of CRAF (unknown origin) compound preincubated for 1 hr in presence of 0.5 uM ATP	B	8.82	pIC50	1.5	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
GtoPdb	Biochemical enzyme inhibition assay.	-	8.85	pIC50	1.4	nM	IC50	J Med Chem (2013) 56: 6478-94 [PMID:23906342]
ChEMBL	Inhibition of N-terminal FLAG-tagged wild type C-RAF (unknown origin) expressed in baculovirus system using GST-MEK1(K96R) as substrate after 20 mins	B	8.85	pIC50	1.4	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
ChEMBL	Inhibition of c-Kit receptor (unknown origin) using biotinylated poly-Glu-Tyr (4:1) as substrate preincubated for 5 mins measured after 12 hrs	B	5	pIC50	>10000	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
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 Src receptor (unknown origin) using biotinylated poly-Glu-Tyr (4:1) as substrate preincubated for 5 mins measured after 12 hrs	B	5	pIC50	>10000	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763]
ChEMBL	Inhibition of TIE2 receptor (unknown origin) using biotinylated poly-Glu-Tyr (4:1) as substrate preincubated for 5 mins measured after 12 hrs	B	6.13	pIC50	740	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
ChEMBL	Inhibition of VEGFR2 (unknown origin) using biotinylated poly-GluTyr (4:1) as substrate pretreated for 5 mins before substrate addition measured after overnight incubation	B	6.8	pIC50	160	nM	IC50	J Med Chem (2013) 56: 6478-6494 [PMID:23906342]

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]