PD166285 [Ligand Id: 8183] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL49120 (TCMDC-140940, PD-0166285)
  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
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  • Glucose transporter in Leishmania mexicana [ChEMBL: CHEMBL3431938] [UniProtKB: O61059]
  • Glucose transporter 1/Glucose transporter in Human [ChEMBL: CHEMBL2535] [GtoPdb: 875] [UniProtKB: P11166]
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  • Hexose transporter 1 in Plasmodium falciparum [ChEMBL: CHEMBL4697] [UniProtKB: O97467]
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  • platelet derived growth factor receptor beta/platelet derived growth factor receptor alpha in Human [GtoPdb: 18041803] [UniProtKB: P09619P16234]
  • platelet derived growth factor receptor beta/platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor in Mouse [ChEMBL: CHEMBL2096980] [GtoPdb: 18041803] [UniProtKB: P05622P26618]
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  • platelet derived growth factor receptor beta in Human [GtoPdb: 1804] [UniProtKB: P09619]
  • platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Mouse [ChEMBL: CHEMBL2749] [GtoPdb: 1804] [UniProtKB: P05622]
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  • WEE1 G2 checkpoint kinase/Serine/threonine-protein kinase WEE1 in Human [ChEMBL: CHEMBL5491] [GtoPdb: 2278] [UniProtKB: P30291]
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  • protein kinase, membrane associated tyrosine/threonine 1/Tyrosine- and threonine-specific cdc2-inhibitory kinase in Human [ChEMBL: CHEMBL3984] [GtoPdb: 2167] [UniProtKB: Q99640]
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  • Tyrosine-protein kinase SRC in Chicken [ChEMBL: CHEMBL3655] [UniProtKB: P00523]
  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Mouse [ChEMBL: CHEMBL3074] [GtoPdb: 2206] [UniProtKB: P05480]
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  • WEE2 oocyte meiosis inhibiting kinase/Wee1-like protein kinase 2 in Human [ChEMBL: CHEMBL5095] [GtoPdb: 2279] [UniProtKB: P0C1S8]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
GtoPdb - - 7.06 pKi 87.5 nM Ki J Pharmacol Exp Ther (1997) 283: 1433-44 [PMID:9400019]
ChEMBL Inhibition of Epidermal growth factor receptor B 4.36 pIC50 44000 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 1931-1935 [PMID:15780636]
ChEMBL Inhibition of human epidermal growth factor receptor B 6.46 pIC50 350 nM IC50 J. Med. Chem. (1998) 41: 1752-1763 [PMID:9599227]
fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
GtoPdb - - 7.41 pKi 39.3 nM Ki J Pharmacol Exp Ther (1997) 283: 1433-44 [PMID:9400019]
ChEMBL Inhibition of fibroblast growth factor receptor (FGFr) B 7.37 pIC50 43 nM IC50 J. Med. Chem. (1998) 41: 3276-3292 [PMID:9703473]
ChEMBL Inhibitory activity against fibroblast growth factor receptor 1 B 7.37 pIC50 43 nM IC50 J. Med. Chem. (2000) 43: 3134-3147 [PMID:10956222]
Glucose transporter in Leishmania mexicana (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3431938] [UniProtKB: O61059]
ChEMBL ST_JUDE_LEISH: Cytotoxicity against transgenic Leishmania Mexicana promastigotes LmGT2 that are glucose transport deficient and complemented with the L. Mexicana glucose transporter 2. Activity is measured by by DNA content using SYBR green in vitro F 4.87 pIC50 13489 nM IC50 St. Jude Leishmania screening dataset.
Glucose transporter 1/Glucose transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2535] [GtoPdb: 875] [UniProtKB: P11166]
ChEMBL ST_JUDE_LEISH: Cytotoxicity against transgenic Leishmania Mexicana promastigotes LmGLUT1 that are glucose transport deficient and complemented with the human glucose transporter GLUT1. Activity is measured by DNA content using SYBR green in vitro F 5 pIC50 9992 nM IC50 St. Jude Leishmania screening dataset.
Hexose transporter 1 in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4697] [UniProtKB: O97467]
ChEMBL ST_JUDE_LEISH: Cytotoxicity against transgenic Leishmania Mexicana promastigotes LmPfHT that are glucose transport deficient and complemented with the Plasmodium falciparum hexose transporter. Activity is measured by by DNA content using SYBR green in vitro F 5.35 pIC50 4496 nM IC50 St. Jude Leishmania screening dataset.
Myelin transcription factor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2331044] [UniProtKB: Q01538]
ChEMBL Binding affinity to human full-length His-tagged Myt1 kinase expressed in HEK293 cells by TR-FRET based binding assay B 8.14 pIC50 7.2 nM IC50 Eur. J. Med. Chem. (2013) 61: 41-48 [PMID:22770610]
platelet derived growth factor receptor beta/platelet derived growth factor receptor alpha in Human [GtoPdb: 18041803] [UniProtKB: P09619P16234]
GtoPdb - - 7.01 pKi 98.3 nM Ki J Pharmacol Exp Ther (1997) 283: 1433-44 [PMID:9400019]
platelet derived growth factor receptor beta/platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor in Mouse (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096980] [GtoPdb: 18041803] [UniProtKB: P05622P26618]
ChEMBL Inhibitory concentration of compound against mouse Platelet-derived growth factor receptor B 7.02 pIC50 96 nM IC50 J. Med. Chem. (1998) 41: 1752-1763 [PMID:9599227]
ChEMBL Inhibition against of platelet-derived growth factor receptor (PDGFr) B 7.1 pIC50 79 nM IC50 J. Med. Chem. (1998) 41: 4365-4377 [PMID:9784112]
ChEMBL Inhibition of PDGF-induced autophosphorylation of PDGF-R in NIH3T3 cells F 8.74 pIC50 1.8 nM IC50 J. Med. Chem. (1998) 41: 3276-3292 [PMID:9703473]
platelet derived growth factor receptor beta in Human [GtoPdb: 1804] [UniProtKB: P09619]
GtoPdb - - 7.01 pKi 98.3 nM Ki J Pharmacol Exp Ther (1997) 283: 1433-44 [PMID:9400019]
platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2749] [GtoPdb: 1804] [UniProtKB: P05622]
ChEMBL Inhibitory concentration was evaluated against Platelet-derived growth factor receptor beta (PDGFr) tyrosine kinase B 7.1 pIC50 79 nM IC50 J. Med. Chem. (1998) 41: 3276-3292 [PMID:9703473]
ChEMBL Inhibitory activity against mouse PDGF beta receptor tyrosine kinase B 7.1 pIC50 79 nM IC50 J. Med. Chem. (2000) 43: 3134-3147 [PMID:10956222]
WEE1 G2 checkpoint kinase/Serine/threonine-protein kinase WEE1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5491] [GtoPdb: 2278] [UniProtKB: P30291]
ChEMBL Binding affinity to recombinant human N-terminal His6-tagged Wee1 kinase domain (291 to 575 residues) expressed in Escherichia coli BL21 (DE3) by isothermal titration calorimetry B 7.96 pKd 11 nM Kd J Med Chem (2017) 60: 7863-7875 [PMID:28792760]
ChEMBL Inhibition of checkpoint kinase Wee1 B 6.78 pIC50 165 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 1931-1935 [PMID:15780636]
GtoPdb - - 7.62 pIC50 24 nM IC50 Cancer Res (2001) 61: 8211-7 [PMID:11719452]
protein kinase, membrane associated tyrosine/threonine 1/Tyrosine- and threonine-specific cdc2-inhibitory kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3984] [GtoPdb: 2167] [UniProtKB: Q99640]
ChEMBL Binding affinity to recombinant human N-terminal His6-tagged Myt1 kinase domain (75 to 361 residues) by isothermal titration calorimetry B 6.61 pKd 247 nM Kd J Med Chem (2017) 60: 7863-7875 [PMID:28792760]
ChEMBL Inhibition of N-[3',6'-dihydroxy-3-oxo-3H-spiro(2-benzofuran-1,9'-xanthen)-5-yl]-N'-[2-(4-{4-[N-(2-chloro-6-methylphenyl)-5-carboxamido]-thiazol-2-yl})-amino-2-methyl-pyrimid-6-yl)piperazinyl]-ethyl]thiourea binding to human PKMYT1 kinase doamin expressed in Escherichia coli BL21 after 120 mins by fluorescence polarization asay B 8.7 pKi 2 nM Ki Bioorg Med Chem (2018) 26: 4014-4024 [PMID:29941193]
ChEMBL Displacement of (6-FAM)KI(pY)VV from PKMYT1 kinase domain (unknown origin) by fluorescence polarization binding assay B 8.7 pKi 2 nM Ki Eur J Med Chem (2019) 161: 479-492 [PMID:30388464]
ChEMBL Displacement of (6-FAM)KI(pY)VV from PKMYT1 kinase domain (unknown origin) by fluorescence polarization binding assay B 8.7 pKi 2 nM Ki Eur J Med Chem (2019) 161: 479-492 [PMID:30388464]
ChEMBL Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay B 9.1 pKi 0.8 nM Ki Bioorg Med Chem (2018) 26: 4014-4024 [PMID:29941193]
ChEMBL Displacement of (6-FAM)KI(pY)VV from full length PKMYT1 (unknown origin) by fluorescence polarization immuno assay B 9.1 pKi 0.8 nM Ki Eur J Med Chem (2019) 161: 479-492 [PMID:30388464]
ChEMBL Inhibition of N-[3',6'-dihydroxy-3-oxo-3H-spiro(2-benzofuran-1,9'-xanthen)-5-yl]-N'-[2-(4-{4-[N-(2-chloro-6-methylphenyl)-5-carboxamido]-thiazol-2-yl})-amino-2-methyl-pyrimid-6-yl)piperazinyl]-ethyl]thiourea binding to human PKMYT1 kinase doamin expressed in Escherichia coli BL21 after 120 mins by fluorescence polarization asay B 7.51 pIC50 31.1 nM IC50 Bioorg Med Chem (2018) 26: 4014-4024 [PMID:29941193]
ChEMBL Displacement of (6-FAM)KI(pY)VV from PKMYT1 kinase domain (unknown origin) by fluorescence polarization binding assay B 7.51 pIC50 31.1 nM IC50 Eur J Med Chem (2019) 161: 479-492 [PMID:30388464]
ChEMBL Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay B 8.1 pIC50 8 nM IC50 Bioorg Med Chem (2018) 26: 4014-4024 [PMID:29941193]
ChEMBL Displacement of (6-FAM)KI(pY)VV from full length PKMYT1 (unknown origin) by fluorescence polarization immuno assay B 8.1 pIC50 8 nM IC50 Eur J Med Chem (2019) 161: 479-492 [PMID:30388464]
GtoPdb - - 8.15 pIC50 7 nM IC50 Cancer Res (2001) 61: 8211-7 [PMID:11719452];
Bioorg Med Chem Lett (2012) 22: 1219-23 [PMID:22189141]
ChEMBL Competitive inhibition of human Myt1 by TR-FRET assay B 8.15 pIC50 7 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 1219-1223 [PMID:22189141]
Tyrosine-protein kinase SRC in Chicken (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3655] [UniProtKB: P00523]
ChEMBL Inhibition of avian c-Src tyrosine kinase B 8.05 pIC50 9 nM IC50 J. Med. Chem. (1998) 41: 3276-3292 [PMID:9703473]
ChEMBL Inhibition of chicken c-Src tyrosine kinase B 8.05 pIC50 9 nM IC50 J. Med. Chem. (1998) 41: 1752-1763 [PMID:9599227]
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
GtoPdb - - 8.08 pKi 8.4 nM Ki J Pharmacol Exp Ther (1997) 283: 1433-44 [PMID:9400019]
ChEMBL Inhibitory activity against avian c-Src tyrosine kinase was determined. B 8.05 pIC50 9 nM IC50 J. Med. Chem. (2000) 43: 3134-3147 [PMID:10956222]
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3074] [GtoPdb: 2206] [UniProtKB: P05480]
ChEMBL Inhibition of mouse c-Src tyrosine kinase B 8.05 pIC50 9 nM IC50 J. Med. Chem. (1998) 41: 4365-4377 [PMID:9784112]
WEE2 oocyte meiosis inhibiting kinase/Wee1-like protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5095] [GtoPdb: 2279] [UniProtKB: P0C1S8]
ChEMBL Binding affinity to recombinant human N-terminal His6-tagged Wee2 kinase domain (202 to 492 residues) expressed in Escherichia coli BL21 (DE3) by isothermal titration calorimetry B 8.3 pKd 5 nM Kd J Med Chem (2017) 60: 7863-7875 [PMID:28792760]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]