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ChEMBL ligand: CHEMBL2436978 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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protein kinase AMP-activated non-catalytic subunit beta 2/protein kinase AMP-activated non-catalytic subunit gamma 1/protein kinase AMP-activated catalytic subunit alpha 2/protein kinase AMP-activated catalytic subunit alpha 1/protein kinase AMP-activated non-catalytic subunit gamma 3/protein kinase AMP-activated non-catalytic subunit gamma 2/protein kinase AMP-activated non-catalytic subunit beta 1/AMP-activated protein kinase, AMPK in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2096907] [GtoPdb: 1544, 1545, 1542, 1541, 1547, 1546, 1543] [UniProtKB: O43741, P54619, P54646, Q13131, Q9UGI9, Q9UGJ0, Q9Y478] | ||||||||
ChEMBL | Inhibition of wild type human AMPK by high throughput ATP-[33P] radiolabeled assay | B | 5.82 | pIC50 | 1512 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
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 wild type human wild type JNK1 by qPCR analysis | B | 5.48 | pIC50 | 3280 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
ChEMBL | Inhibition of wild type human JNK1 by high throughput [33P]-ATP radiolabeled assay | B | 5.49 | pIC50 | 3200 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493] | ||||||||
ChEMBL | Inhibition of wild type human CDK1 by high throughput ATP-[33P] radiolabeled assay | B | 5.95 | pIC50 | 1125 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941] | ||||||||
ChEMBL | Inhibition of wild type human CDK2 by high throughput ATP-[33P] radiolabeled assay | B | 5.93 | pIC50 | 1180 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
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 wild type human GSK3B by high throughput ATP-[33P] radiolabeled assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
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 wild type human c-MET by high throughput ATP-[33P] radiolabeled assay | B | 6.75 | pIC50 | 177 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
ChEMBL | Inhibition of human ERG tail current transfected in HEK293 cells by patch clamp assay | B | 4.68 | pIC50 | 21000 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
component of inhibitor of nuclear factor kappa B kinase complex/Inhibitor of nuclear factor kappa B kinase alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3476] [GtoPdb: 1989] [UniProtKB: O15111] | ||||||||
ChEMBL | Inhibition of wild type human IKKa by high throughput ATP-[33P] radiolabeled assay | B | 6.23 | pIC50 | 591 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
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 wild type human IKKb by high throughput ATP-[33P] radiolabeled assay | B | 6.59 | pIC50 | 257 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
Insulin-like growth factor I receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069] | ||||||||
ChEMBL | Inhibition of wild type human IGF1R by high throughput ATP-[33P] radiolabeled assay | B | 6.51 | pIC50 | 307 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213] | ||||||||
ChEMBL | Inhibition of wild type human IR by high throughput ATP-[33P] radiolabeled assay | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
leucine rich repeat kinase 2/Leucine-rich repeat serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075104] [GtoPdb: 2059] [UniProtKB: Q5S007] | ||||||||
ChEMBL | Inhibition of human wild type LRRK2 by qPCR analysis | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
GtoPdb | - | - | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2013) 56: 8032-48 [PMID:24044867] |
mitogen-activated protein kinase 1/MAP kinase ERK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482] | ||||||||
ChEMBL | Inhibition of wild type human ERK2 by high throughput ATP-[33P] radiolabeled assay | B | 5.2 | pIC50 | 6290 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] | ||||||||
ChEMBL | Inhibition of wild type human P38a by high throughput ATP-[33P] radiolabeled assay | B | 4.92 | pIC50 | 12050 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
mitogen-activated protein kinase kinase kinase 10/Mitogen-activated protein kinase kinase kinase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2873] [GtoPdb: 2070] [UniProtKB: Q02779] | ||||||||
ChEMBL | Inhibition of MLK2 (unknown origin) | B | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
GtoPdb | - | - | 7.38 | pIC50 | 42 | nM | IC50 | J Med Chem (2013) 56: 8032-48 [PMID:24044867] |
mitogen-activated protein kinase kinase kinase 11/Mitogen-activated protein kinase kinase kinase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2708] [GtoPdb: 2071] [UniProtKB: Q16584] | ||||||||
GtoPdb | - | - | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2013) 56: 8032-48 [PMID:24044867] |
ChEMBL | Inhibition of MLK3 (unknown origin) after 20 mins by scintillation counting analysis in presence of [33P]-ATP | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
mitogen-activated protein kinase kinase kinase 11/Mitogen-activated protein kinase kinase kinase 11 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2434817] [GtoPdb: 2071] [UniProtKB: Q80XI6] | ||||||||
ChEMBL | Inhibition of MLK3 in mouse BV2 cells assessed as inhibition of LPS-induced TNFalpha release after 8 hrs by ELISA | B | 6.34 | pIC50 | 460 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
mitogen-activated protein kinase kinase kinase 2/Mitogen-activated protein kinase kinase kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5914] [GtoPdb: 2077] [UniProtKB: Q9Y2U5] | ||||||||
ChEMBL | Inhibition of wild type human MEKK2 by high throughput ATP-[33P] radiolabeled assay | B | 6.18 | pIC50 | 661 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
GtoPdb | - | - | 6.18 | pIC50 | 661 | nM | IC50 | J Med Chem (2013) 56: 8032-48 [PMID:24044867] |
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] | ||||||||
GtoPdb | - | - | 7.72 | pIC50 | 19 | nM | IC50 | J Med Chem (2013) 56: 8032-48 [PMID:24044867] |
ChEMBL | Inhibition of MLK1 (unknown origin) | B | 7.72 | pIC50 | 19 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629] | ||||||||
ChEMBL | Inhibition of wild type human TRKA by high throughput ATP-[33P] radiolabeled assay | B | 7.07 | pIC50 | 85 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
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 wild type human TRKB by high throughput ATP-[33P] radiolabeled assay | B | 6.66 | pIC50 | 217 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
Protein delta homolog 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5671] [UniProtKB: P80370] | ||||||||
ChEMBL | Binding affinity to human wild type DLK by qPCR analysis | B | 7.15 | pKd | 70 | nM | Kd | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
ChEMBL | Inhibition of human wild type DLK by qPCR analysis | B | 6.82 | pIC50 | 150 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
Rho associated coiled-coil containing protein kinase 1/Rho-associated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3231] [GtoPdb: 1503] [UniProtKB: Q13464] | ||||||||
ChEMBL | Inhibition of wild type human ROCK1 by high throughput ATP-[33P] radiolabeled assay | B | 5.99 | pIC50 | 1030 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
Rho associated coiled-coil containing protein kinase 2/Rho-associated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2973] [GtoPdb: 1504] [UniProtKB: O75116] | ||||||||
ChEMBL | Inhibition of wild type human ROCK2 by high throughput ATP-[33P] radiolabeled assay | B | 6.95 | pIC50 | 111 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965] | ||||||||
ChEMBL | Inhibition of wild type human Aurora kinase A by high throughput ATP-[33P] radiolabeled assay | B | 6.97 | pIC50 | 108 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4] | ||||||||
ChEMBL | Inhibition of wild type human Aurora kinase B by high throughput ATP-[33P] radiolabeled assay | B | 6.91 | pIC50 | 123 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
aurora kinase C/Serine/threonine-protein kinase Aurora-C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3935] [GtoPdb: 1938] [UniProtKB: Q9UQB9] | ||||||||
ChEMBL | Inhibition of wild type human Aurora kinase C kinase by high throughput ATP-[33P] radiolabeled assay | B | 6.54 | pIC50 | 290 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
serum/glucocorticoid regulated kinase 1/Serine/threonine-protein kinase Sgk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2343] [GtoPdb: 1534] [UniProtKB: O00141] | ||||||||
ChEMBL | Inhibition of wild type human SGK1 by high throughput ATP-[33P] radiolabeled assay | B | 6.7 | pIC50 | 201 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
TRAF2 and NCK interacting kinase/TRAF2- and NCK-interacting kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4527] [GtoPdb: 2244] [UniProtKB: Q9UKE5] | ||||||||
ChEMBL | Inhibition of TNIK (unknown origin) | B | 8.28 | pIC50 | 5.2 | nM | IC50 | Bioorg Med Chem Lett (2021) 33: 127749-127749 [PMID:33340663] |
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 | Inhibition of wild type human ABL1 by high throughput ATP-[33P] radiolabeled assay | B | 8.17 | pIC50 | 6.8 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
ChEMBL | Inhibition of wild type human ABL1 T315I mutant by high throughput ATP-[33P] radiolabeled assay | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
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 wild type human LCK by high throughput ATP-[33P] radiolabeled assay | B | 6.48 | pIC50 | 333 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
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-L-stimulated wild type full length human FLT3 autophosphorylation expressed in MEF preincubated for 90 mins followed by FLT3-L stimulation measured after 5 mins by ELISA | B | 6.25 | pIC50 | 560 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
ChEMBL | Inhibition of wild type human FLT3 by high throughput ATP-[33P] radiolabeled assay | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
GtoPdb | - | - | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2013) 56: 8032-48 [PMID:24044867] |
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 wild type human SRC by high throughput ATP-[33P] radiolabeled assay | B | 5.36 | pIC50 | 4330 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405] | ||||||||
ChEMBL | Inhibition of wild type human SYK by high throughput ATP-[33P] radiolabeled assay | B | 6.14 | pIC50 | 731 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
zeta chain of T cell receptor associated protein kinase 70/Tyrosine-protein kinase ZAP-70 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2803] [GtoPdb: 2285] [UniProtKB: P43403] | ||||||||
ChEMBL | Inhibition of wild type human ZAP70 by high throughput ATP-[33P] radiolabeled assay | B | 5.3 | pIC50 | 5050 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948] | ||||||||
ChEMBL | Inhibition of wild type human FLT1 by high throughput ATP-[33P] radiolabeled assay | B | 7.41 | pIC50 | 39 | nM | IC50 | J Med Chem (2013) 56: 8032-8048 [PMID:24044867] |
death associated protein kinase 3 in Human [GtoPdb: 2004] [UniProtKB: O43293] | ||||||||
GtoPdb | - | - | 6.82 | pIC50 | 150 | nM | IC50 | J Med Chem (2013) 56: 8032-48 [PMID:24044867] |
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]