leniolisib [Ligand Id: 9424] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3643413 (Cdz-173 free base, Cdz173 free base, CDZ-173-NX, CDZ173-NX, Leniolisib) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| phosphodiesterase 4D/3`,5`-cyclic-AMP phosphodiesterase 4D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499] | ||||||||
| ChEMBL | Inhibition of recombinant human PDE4D | B | 5.33 | pIC50 | 4700 | nM | IC50 | ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947] |
| ChEMBL | Selectivity interaction (Phosphodiesterase 4D, human recombinant ) EUB0000877a PDE4D | B | 5.33 | pIC50 | 4700 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Selectivity interaction (Serotonin 5HT1A Calcium flux assay, agonist and antagonist mode ) EUB0000877a HTR1A | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| 5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Selectivity interaction (Serotonin 5HT2A Calcium flux assay, agonist and antagonist mode ) EUB0000877a HTR2A | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| 5-HT2B receptor/5-hydroxytryptamine receptor 2B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| ChEMBL | Selectivity interaction (Serotonin 5HT2B Calcium flux assay, agonist mode ) EUB0000877a HTR2B | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of 5-HT2B (unknown origin) by calcium flux assay | F | 5.11 | pIC50 | 7700 | nM | IC50 | ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947] |
| ChEMBL | Selectivity interaction (Serotonin 5HT2B Calcium flux assay, antagonist mode ) EUB0000877a HTR2B | B | 5.11 | pIC50 | 7700 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| 5-HT3A/5-hydroxytryptamine receptor 3A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098] | ||||||||
| ChEMBL | Selectivity interaction (Serotonin 5HT3 receptor assay, human recombinant ) EUB0000877a HTR3A | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| nicotinic acetylcholine receptor α1 subunit/Acetylcholine receptor subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4808] [GtoPdb: 462] [UniProtKB: P02708] | ||||||||
| ChEMBL | Selectivity interaction (Nicotinic (CNS) Receptor binding in human IMR32 cells ) EUB0000877a CHRNA1 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| Acylglycerol kinase, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2417354] [UniProtKB: Q53H12] | ||||||||
| ChEMBL | Selectivity interaction (Adrenergic Alpha 2C receptor assay, human recombinant ) EUB0000877a AGK | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| A1 receptor/Adenosine receptor A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542] | ||||||||
| ChEMBL | Selectivity interaction (Adenosine 1 receptor binding assay, human recombinant) EUB0000877a ADORA1 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| A2A receptor/Adenosine receptor A2a in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
| ChEMBL | Selectivity interaction (Adenosine 2A receptor binding assay, human recombinant ) EUB0000877a ADORA2A | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| A3 receptor/Adenosine receptor A3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
| ChEMBL | Selectivity interaction (Adenosine 3 receptor binding assay, human recombinant ) EUB0000877a ADORA3 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a ALK | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| α1A-adrenoceptor/Alpha-1A adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
| ChEMBL | Selectivity interaction (Alpha1A calcium flux assay ) EUB0000877a ADRA1A | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| α2A-adrenoceptor/Alpha-2A adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| ChEMBL | Selectivity interaction (Alpha2A calcium flux assay ) EUB0000877a ADRA2A | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| Monoamine oxidase A/Amine oxidase [flavin-containing] A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1951] [GtoPdb: 2489] [UniProtKB: P21397] | ||||||||
| ChEMBL | Selectivity interaction (Monoamine Oxidase A, human recombinant baculovirus ) EUB0000877a MAOA | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| aurora kinase A/Aurora kinase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a STK6 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| B2 receptor/B2 bradykinin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3157] [GtoPdb: 42] [UniProtKB: P30411] | ||||||||
| ChEMBL | Selectivity interaction (Bradykinin 2 receptor binding assay, human recombinant ) EUB0000877a BDKRB2 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588] | ||||||||
| ChEMBL | Selectivity interaction (Beta 1 adrenergic receptor assay, human recombinant ) EUB0000877a ADRB1 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550] | ||||||||
| ChEMBL | Selectivity interaction (Adrenergic Alpha 2B receptor assay, human recombinant ) EUB0000877a ADRB2 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (Beta 2 adrenergic receptor assay, human recombinant ) EUB0000877a ADRB2 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| protein kinase, cAMP-dependent, catalytic, alpha subunit/cAMP-dependent protein kinase catalytic subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4101] [GtoPdb: 1476] [UniProtKB: P17612] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a PRKACA | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| CB1 receptor/Cannabinoid receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554] | ||||||||
| ChEMBL | Selectivity interaction (Cannabinoid CB1 calcium flux assay, agonist and antagonist mode ) EUB0000877a CNR1 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| Cellular tumor antigen p53 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4096] [UniProtKB: P04637] | ||||||||
| ChEMBL | Inhibition of p53 in human HCT116 cells assessed as reduction in nutlin-induced p53 transcriptional response by FRET assay | B | 5.52 | pIC50 | >3000 | nM | IC50 | ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947] |
| phosphodiesterase 3A/cGMP-inhibited 3`,5`-cyclic phosphodiesterase 3A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL241] [GtoPdb: 1298] [UniProtKB: Q14432] | ||||||||
| ChEMBL | Selectivity interaction (Phosphodiesterase 3 from human platelets ) EUB0000877a PDE3A | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| CCK1 receptor/Cholecystokinin receptor type A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1901] [GtoPdb: 76] [UniProtKB: P32238] | ||||||||
| ChEMBL | Selectivity interaction (Cholecystokinin A receptor binding assay, human recombinant ) EUB0000877a CCKAR | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a CDK4 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| Cyclin-dependent kinase inhibitor 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4680027] [UniProtKB: P42771] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a CDKN2A | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| D1 receptor/D(1A) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
| ChEMBL | Selectivity interaction (Dopamine D1 - cAMP agonist mode ) EUB0000877a DRD1 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| D2 receptor/D(2) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Selectivity interaction (Dopamine D2 receptor assay, human recombinant ) EUB0000877a DRD2 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| D3 receptor/D(3) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Selectivity interaction (Dopamine D3 receptor assay, human recombinant ) EUB0000877a DRD3 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| δ receptor/Delta-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
| ChEMBL | Selectivity interaction (Opiate Delta receptor assay, human recombinant ) EUB0000877a OPRD1 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase catalytic subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527] | ||||||||
| ChEMBL | Inhibition of DNA-PK (unknown origin) using peptide substrate assessed as reduction in incorporation of radioactive 33p into substrate by liquid scintillation counting method | B | 6.06 | pIC50 | 880 | nM | IC50 | ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947] |
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a PRKDC | B | 6.06 | pIC50 | 880 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ETA receptor/Endothelin-1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101] | ||||||||
| ChEMBL | Selectivity interaction (Endothelin A receptor binding assay, human recombinant ) EUB0000877a EDNRA | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| EPH receptor A4/Ephrin type-A receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3988] [GtoPdb: 1824] [UniProtKB: P54764] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a EPHA4 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| EPH receptor B4/Ephrin type-B receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5147] [GtoPdb: 1833] [UniProtKB: P54760] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a EPHB4 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| epidermal growth factor receptor/Epidermal growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a EGFR | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| Estrogen receptor-α/Estrogen receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372] | ||||||||
| ChEMBL | Selectivity interaction (Estrogen alpha receptor binding assay, human recombinant ) EUB0000877a ESR1 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a FGFR3 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3973] [GtoPdb: 1811] [UniProtKB: P22455] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a FGFR4 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| CCK2 receptor/Gastrin/cholecystokinin type B receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL298] [GtoPdb: 77] [UniProtKB: P32239] | ||||||||
| ChEMBL | Selectivity interaction (Cholecystokinin B receptor binding assay, human recombinant ) EUB0000877a CCKBR | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150] | ||||||||
| ChEMBL | Selectivity interaction (Glucocorticoid receptor binding assay, human recombinant ) EUB0000877a NR3C1 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a GSK3B | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ghrelin receptor/Growth hormone secretagogue receptor type 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4616] [GtoPdb: 246] [UniProtKB: Q92847] | ||||||||
| ChEMBL | Selectivity interaction (Ghrelin receptor binding assay, human recombinant ) EUB0000877a GHRL | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a MET | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
| ChEMBL | Selectivity interaction (Histamine H1 receptor assay, human recombinant ) EUB0000877a HRH1 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1] | ||||||||
| ChEMBL | Selectivity interaction (Human histamine H3 receptor binding assay ) EUB0000877a HRH3 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| Insulin-like growth factor I receptor/Insulin-like growth factor 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a IGF1R | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a INSR | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| κ receptor/Kappa-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| ChEMBL | Selectivity interaction (Opiate Kappa receptor assay, human recombinant ) EUB0000877a OPRK1 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a MAPKAPK2 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| MAPK activated protein kinase 5/MAP kinase-activated protein kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3094] [GtoPdb: 2096] [UniProtKB: Q8IW41] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a MAPKAPK5 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| MAPK interacting serine/threonine kinase 2/MAP kinase-interacting serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a MKNK2 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| KIT proto-oncogene, receptor tyrosine kinase/Mast/stem cell growth factor receptor Kit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a KIT | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| MC3 receptor/Melanocortin receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4644] [GtoPdb: 284] [UniProtKB: P41968] | ||||||||
| ChEMBL | Selectivity interaction (Melanocortin MC3 receptor binding assay, human recombinant ) EUB0000877a MC3R | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| mitogen-activated protein kinase 1/Mitogen-activated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a MAPK1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| mitogen-activated protein kinase 14/Mitogen-activated protein kinase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a MAPK14 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| mitogen-activated protein kinase kinase kinase 8/Mitogen-activated protein kinase kinase kinase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4899] [GtoPdb: 2083] [UniProtKB: P41279] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a MAP3K8 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| motilin receptor/Motilin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2203] [GtoPdb: 297] [UniProtKB: O43193] | ||||||||
| ChEMBL | Selectivity interaction (Motilin receptor binding assay, human recombinant ) EUB0000877a MLNR | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
| ChEMBL | Selectivity interaction (Muscarinic M1 receptor assay, human recombinant ) EUB0000877a CHRM1 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
| ChEMBL | Selectivity interaction (Muscarinic M2 Calcium flux assay, agonist and antagonist mode ) EUB0000877a CHRM2 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
| ChEMBL | Selectivity interaction (Muscarinic M3 receptor assay, human recombinant ) EUB0000877a CHRM3 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| μ receptor/Mu-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| ChEMBL | Selectivity interaction (Opioid Mu GTPgS agonist assay ) EUB0000877a OPRM1 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| Y1 receptor/Neuropeptide Y receptor type 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4777] [GtoPdb: 305] [UniProtKB: P25929] | ||||||||
| ChEMBL | Selectivity interaction (Neuropeptide Y Y1 receptor binding assay, human recombinant ) EUB0000877a NPY1R | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| tyrosine kinase 2/Non-receptor tyrosine-protein kinase TYK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a TYK2 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| Pregnane X receptor/Nuclear receptor subfamily 1 group I member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3401] [GtoPdb: 606] [UniProtKB: O75469] | ||||||||
| ChEMBL | Selectivity interaction (Pregnane X Receptor (PXR, SXR) binding, human recombinant ) EUB0000877a NR1I2 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Selectivity interaction (PXR Receptor agonist/antagonist assay: TR-FRET human recombinant ) EUB0000877a NR1I2 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| phosphatidylinositol 3-kinase catalytic subunit type 3/Phosphatidylinositol 3-kinase catalytic subunit type 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075165] [GtoPdb: 2152] [UniProtKB: Q8NEB9] | ||||||||
| ChEMBL | Inhibition of Vps34 (unknown origin) using phosphatidyl inositol/n-Octyl-glucoside as substrate measured after 30 mins by KinaseGlo assay | B | 5.04 | pIC50 | >9100 | nM | IC50 | ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947] |
| ChEMBL | Selectivity interaction (Kinase panel (ADP-Glow assay)) EUB0000877a PIK3C3 | B | 5.04 | pIC50 | >9100 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336] | ||||||||
| GtoPdb | In vitro enzyme assay | - | 6.58 | pIC50 | 262 | nM | IC50 | WO2012004299. Tetrahydro-pyrido-pyrimidine derivatives (2012) |
| ChEMBL | Enzyme Assay: Test of Lipid Kinase Activity: The kinase reaction is performed in a final volume of 50 μl per well of a half area COSTAR, 96 well plate. The final concentrations of ATP and phosphatidyl inositol in the assay are 5 μM and 6 μg/mL, respectively. The reaction is started by the addition of PI3 kinase, e.g. PI3 kinase δ. Refer to the patent for more info. | B | 6.58 | pIC50 | 262 | nM | IC50 | US-8653092-B2. Tetrahydro-pyrido-pyrimidine derivatives (2014) |
| ChEMBL | Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate measured after 1 hr in presence of ATP by ADP-glo luminescence assay | B | 7.12 | pIC50 | 75.5 | nM | IC50 | J Med Chem (2022) 65: 8011-8028 [PMID:35609190] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2499] [GtoPdb: 2153] [UniProtKB: P42337] | ||||||||
| ChEMBL | Inhibition of PI3Kalpha in IGF-1 stimulated mouse C2C12 cells incubated for 10 mins by AlphaLISA assay | B | 4.71 | pIC50 | 19628.2 | nM | IC50 | J Med Chem (2022) 65: 8011-8028 [PMID:35609190] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3145] [GtoPdb: 2154] [UniProtKB: P42338] | ||||||||
| ChEMBL | Inhibition of PI3Kbeta in LPA stimulated human PC-3 cells incubated for 10 mins by AlphaLISA assay | B | 5.57 | pIC50 | 2683.7 | nM | IC50 | J Med Chem (2022) 65: 8011-8028 [PMID:35609190] |
| ChEMBL | Inhibition of PI3Kbeta (unknown origin) using PIP2 as substrate measured after 1 hr in presence of ATP by ADP-glo luminescence assay | B | 6.44 | pIC50 | 363 | nM | IC50 | J Med Chem (2022) 65: 8011-8028 [PMID:35609190] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329] | ||||||||
| ChEMBL | Inhibition of PI3Kdelta in anti-CD3/CD28 stimulated human PBMC derived CD4-positive T cells assessed as reduction in cell proliferation by measuring [3H]thymidine incorporation by beta counting method | B | 5.94 | pIC50 | 1150 | nM | IC50 | ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947] |
| ChEMBL | Inhibition of PI3Kdelta in 90% human whole blood assessed as reduction in anti-IgM/IL4 stimulated CD86 expression pretreated for 1 hr followed by anti-IgM/IL4 stimulation after 24 hrs by flow cytometric analysis | B | 6.69 | pIC50 | 202 | nM | IC50 | ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947] |
| ChEMBL | Inhibition of PI3Kdelta in 90% human whole blood assessed as reduction in anti-IgM/IL4 stimulated CD69 expression pretreated for 1 hr followed by anti-IgM/IL4 stimulation after 24 hrs by flow cytometric analysis | B | 6.71 | pIC50 | 193 | nM | IC50 | ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947] |
| ChEMBL | Inhibition of PI3Kdelta in anti-CD3 stimulated human PBMC assessed as reduction in cell proliferation by measuring [3H]thymidine incorporation pretreated for 1 hr followed by anti-CD3 addition measured last 16 hrs of 56 hrs incubation by beta counting method | B | 6.8 | pIC50 | 159 | nM | IC50 | ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947] |
| ChEMBL | Inhibition of PI3Kdelta in human B cells assessed as reduction in anti-IgM-induced AKT phosphorylation at ser473 residue pretreated for 1.5 hrs followed by anti-IgM stimulation after 20 mins by flow cytometric analysis | B | 6.84 | pIC50 | 144 | nM | IC50 | ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947] |
| ChEMBL | Inhibition of PI3Kdelta in anti-CD3/CD28 stimulated human PBMC derived CD4-positive T cells assessed as reduction in T cell differentiation to Th2 cells by measuring IL-13 level after 72 hrs by ELISA | B | 7.02 | pIC50 | 95 | nM | IC50 | ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947] |
| ChEMBL | Inhibition of PI3Kdelta in human PBMC assessed as reduction in cell proliferation by measuring [3H]thymidine incorporation measured last 16 hrs of 4 days incubation by beta counting based mixed lymphocyte reaction assay | B | 7.1 | pIC50 | 79 | nM | IC50 | ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947] |
| ChEMBL | Inhibition of PI3Kdelta in anti-CD3/CD28 stimulated human PBMC derived CD4-positive T cells assessed as reduction in T cell differentiation to Th17 cells by measuring IL-17A level after 72 hrs by ELISA | B | 7.14 | pIC50 | 73 | nM | IC50 | ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947] |
| ChEMBL | Inhibition of PI3Kdelta in IgM stimulated human Raji cells incubated for 10 mins by AlphaLISA assay | B | 7.2 | pIC50 | 62.8 | nM | IC50 | J Med Chem (2022) 65: 8011-8028 [PMID:35609190] |
| ChEMBL | Inhibition of recombinant human myristoylated PI3Kdelta catalytic domain expressed in Rat1 cells assessed as reduction in Akt phosphorylation at Ser47 residue after 1 hr by alpha screen Surefire assay | B | 7.25 | pIC50 | 56 | nM | IC50 | ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947] |
| ChEMBL | Affinity Phenotypic Cellular interaction: (Inhibition of p-AKT(Ser473) formation (AlphaScreenxc2xae SureFirexc2xae assay, Rat-1 cells)) EUB0000877a PIK3CD | F | 7.25 | pIC50 | 56 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Enzyme Assay: Test of Lipid Kinase Activity: The kinase reaction is performed in a final volume of 50 μl per well of a half area COSTAR, 96 well plate. The final concentrations of ATP and phosphatidyl inositol in the assay are 5 μM and 6 μg/mL, respectively. The reaction is started by the addition of PI3 kinase, e.g. PI3 kinase δ. Refer to the patent for more info. | B | 7.64 | pIC50 | 23 | nM | IC50 | US-8653092-B2. Tetrahydro-pyrido-pyrimidine derivatives (2014) |
| GtoPdb | In vitro enzyme assay | - | 7.64 | pIC50 | 23 | nM | IC50 | WO2012004299. Tetrahydro-pyrido-pyrimidine derivatives (2012) |
| ChEMBL | Inhibition of PI3Kdelta (unknown origin) using phosphatidyl inositol as substrate measured after 60 mins by Alexa Fluor647-labelled ADP tracer based TR-FRET assay | B | 7.96 | pIC50 | 11 | nM | IC50 | ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947] |
| ChEMBL | Affinity Biochemical interaction: (Adaptatm TR-FRET assay) EUB0000877a PIK3CD | B | 7.96 | pIC50 | 11 | nM | IC50 | Affinity Biochemical Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of PI3Kdelta (unknown origin) using PIP2 as substrate measured after 1 hr in presence of ATP by ADP-glo luminescence assay | B | 8.82 | pIC50 | 1.5 | nM | IC50 | J Med Chem (2022) 65: 8011-8028 [PMID:35609190] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2216745] [GtoPdb: 2155] [UniProtKB: O35904] | ||||||||
| ChEMBL | Inhibition of PI3Kdelta in anti-CD3/CD28 stimulated mouse CD4-positive T cells assessed as reduction in T cell differentiation to Th17 cells by measuring IL-17A level after 72 hrs by ELISA | B | 7 | pIC50 | 101 | nM | IC50 | ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947] |
| ChEMBL | Inhibition of PI3Kdelta in Balb/c mouse splenocytes assessed as reduction in anti-IgM stimulated CD86 expression pretreated for 1 hr followed by anti-IgM stimulation after 24 hrs by flow cytometric analysis | B | 7.32 | pIC50 | 48 | nM | IC50 | ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947] |
| ChEMBL | Inhibition of PI3Kdelta in mouse spleen cells assessed as reduction in cell proliferation by measuring [3H]thymidine incorporation by beta counting based mixed lymphocyte reaction assay | B | 7.48 | pIC50 | 33 | nM | IC50 | ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947] |
| ChEMBL | Inhibition of PI3Kdelta in anti-CD3/CD28 stimulated mouse CD4-positive T cells assessed as reduction in T cell differentiation to Th2 cells by measuring IL-13 level after 72 hrs by ELISA | B | 8 | pIC50 | 10 | nM | IC50 | ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947] |
| ChEMBL | Inhibition of PI3Kdelta in mouse B cells assessed as reduction in anti-IgM-induced cell proliferation measured last 16 hrs of 88 hrs incubation by [3H]thymidine incorporation assay | B | 8.15 | pIC50 | 7 | nM | IC50 | ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736] | ||||||||
| ChEMBL | Inhibition of PI3Kgamma in human U937 cells assessed as reduction in MIP-1 alpha stimulated ATK phosphorylation at ser473 residue pretreated for 30 mins followed by MIP-1 alpha addition measured after 3 mins by fluorescence assay | B | 5.13 | pIC50 | >7400 | nM | IC50 | ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947] |
| ChEMBL | Inhibition of PI3Kgamma (unknown origin) using phosphatidyl inositol as substrate measured after 30 mins by Alexa Fluor647-labelled ADP tracer based TR-FRET assay | B | 5.65 | pIC50 | 2230 | nM | IC50 | ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947] |
| ChEMBL | Inhibition of PI3Kgamma (unknown origin) using PIP2 as substrate measured after 1 hr in presence of ATP by ADP-glo luminescence assay | B | 6.04 | pIC50 | 902 | nM | IC50 | J Med Chem (2022) 65: 8011-8028 [PMID:35609190] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189158] [GtoPdb: 2156] [UniProtKB: Q9JHG7] | ||||||||
| ChEMBL | Inhibition of PI3Kgamma in C57/Bl6 mouse BMMC assessed as reduction in adenosine stimulated ATK phosphorylation at ser473 residue pretreated for 30 mins followed by adenosine addition measured after 3 minutes | B | 5.11 | pIC50 | 7800 | nM | IC50 | ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947] |
| ChEMBL | Inhibition of PI3Kgamma in C5a stimulated mouse RAW264.7 cells incubated for 10 mins by AlphaLisa assay | B | 5.39 | pIC50 | 4037.4 | nM | IC50 | J Med Chem (2022) 65: 8011-8028 [PMID:35609190] |
| phosphatidylinositol 4-kinase alpha/Phosphatidylinositol 4-kinase alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3667] [GtoPdb: 2148] [UniProtKB: P42356] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (radiometric assay)) EUB0000877a PI4KA | B | 5.04 | pIC50 | >9100 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| phosphatidylinositol 4-kinase beta/Phosphatidylinositol 4-kinase beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3268] [GtoPdb: 2149] [UniProtKB: Q9UBF8] | ||||||||
| ChEMBL | Inhibition of PI4Kbeta (unknown origin) using phosphatidyl inositol/n-Octyl-glucoside as substrate measured after 30 mins by KinaseGlo assay | B | 5.04 | pIC50 | >9100 | nM | IC50 | ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947] |
| platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a PDGFRA | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| Progesterone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401] | ||||||||
| ChEMBL | Selectivity interaction (Progesteron receptor agonist/antagonist FRET assay, human recombinant) EUB0000877a PGR | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| COX-2 /Prostaglandin G/H synthase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354] | ||||||||
| ChEMBL | Selectivity interaction (COX-2 assay, human recombinant ) EUB0000877a PTGS2 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| protein kinase C alpha/Protein kinase C alpha type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a PRKCA | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| protein kinase C theta/Protein kinase C theta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3920] [GtoPdb: 1488] [UniProtKB: Q04759] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a PRKCQ | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ret proto-oncogene/Proto-oncogene tyrosine-protein kinase receptor Ret in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a RET | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| pyruvate dehydrogenase kinase 1/[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4766] [GtoPdb: 2915] [UniProtKB: Q15118] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a PDK1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| AKT serine/threonine kinase 1/RAC-alpha serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a AKT1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| erb-b2 receptor tyrosine kinase 2/Receptor tyrosine-protein kinase erbB-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a ERBB2 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| 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 | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a ROCK2 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345] | ||||||||
| ChEMBL | Inhibition of mTOR (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 8011-8028 [PMID:35609190] |
| ChEMBL | Inhibition of recombinant mTOR (unknown origin) using 4EBP1 as substrate by TR-FRET assay | B | 5.04 | pIC50 | >9100 | nM | IC50 | ACS Med Chem Lett (2017) 8: 975-980 [PMID:28947947] |
| ChEMBL | Selectivity interaction (Kinase panel (antibody-dependent TR-FRET assay, phosphorylation of 4EBP-1 catalyzed by recombinant mTOR)) EUB0000877a MTOR | B | 5.04 | pIC50 | >9100 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| protein kinase N1/Serine/threonine-protein kinase N1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3384] [GtoPdb: 1520] [UniProtKB: Q16512] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a PKN1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| protein kinase N2/Serine/threonine-protein kinase N2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3032] [GtoPdb: 1521] [UniProtKB: Q16513] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a PKN2 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| DAT/Sodium-dependent dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] | ||||||||
| ChEMBL | Selectivity interaction (Dopamine Transporter assay, human recombinant ) EUB0000877a SLC6A3 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| NET/Sodium-dependent noradrenaline transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
| ChEMBL | Selectivity interaction (Norepinephrine Transporter assay, human recombinant ) EUB0000877a SLC6A2 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| SERT/Sodium-dependent serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
| ChEMBL | Selectivity interaction (Serotonin transporter site assay, human recombinant ) EUB0000877a SLC6A4 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| TP receptor/Thromboxane A2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2069] [GtoPdb: 346] [UniProtKB: P21731] | ||||||||
| ChEMBL | Selectivity interaction (Thromboxane A2 receptor binding assay, human recombinant) EUB0000877a TBXA2R | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| AT1 receptor/Type-1 angiotensin II receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556] | ||||||||
| ChEMBL | Selectivity interaction (Angiotensin II AT1 receptor binding assay, human recombinant ) EUB0000877a AGTR1 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a ABL1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a BTK | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a JAK1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a JAK2 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a JAK3 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lck in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a LCK | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a AXL | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a SYK | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| 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 | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a ZAP70 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (33PanQinase(R) Activity Assay)) EUB0000877a KDR | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| V2 receptor/Vasopressin V2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1790] [GtoPdb: 368] [UniProtKB: P30518] | ||||||||
| ChEMBL | Selectivity interaction (Vasopressin V2 receptor binding assay, human recombinant ) EUB0000877a AVPR2 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Selectivity interaction (HERG dofetilide binding assay, human recombinant ) EUB0000877a KCNH2 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
ChEMBL data shown on this page come from version 36:
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]
