URMC-099 [Ligand Id: 8106] activity data from GtoPdb and ChEMBL
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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 |
|---|---|---|---|---|---|---|---|---|
| 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
