PD166285 [Ligand Id: 8183] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL49120 (PD-0166285, TCMDC-140940) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| activin A receptor type 1/Activin receptor type-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5903] [GtoPdb: 1785] [UniProtKB: Q04771] | ||||||||
| ChEMBL | Inhibition of human ALK2 using casein as substrate incubated for 30 mins in presence of [gamma33P]ATP by radiometric hotspot kinase assay | B | 7.68 | pIC50 | 21 | nM | IC50 | Eur J Med Chem (2021) 215: 113252-113252 [PMID:33601309] |
| cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493] | ||||||||
| ChEMBL | Inhibition of CDK1 (unknown origin) | B | 7 | pIC50 | <100 | nM | IC50 | J Med Chem (2020) 63: 14151-14183 [PMID:33135887] |
| ChEMBL | Inhibition of MYT1 (unknown origin) | B | 7 | pIC50 | <100 | nM | IC50 | J Med Chem (2020) 63: 14151-14183 [PMID:33135887] |
| 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] |
| ChEMBL | Inhibition of EGFR (unknown origin) | B | 7 | pIC50 | <100 | nM | IC50 | J Med Chem (2020) 63: 14151-14183 [PMID:33135887] |
| 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 FGFR1 (unknown origin) | B | 7 | pIC50 | <100 | nM | IC50 | J Med Chem (2020) 63: 14151-14183 [PMID:33135887] |
| 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] |
| nucleotide binding oligomerization domain containing 2/Nucleotide-binding oligomerization domain-containing protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293266] [GtoPdb: 1763] [UniProtKB: Q9HC29] | ||||||||
| ChEMBL | Inhibition of human NOD2 expressed in HEK-blue cells coexpressing NFkappaB-SEAP reporter assessed as reduction in L18-MDP-induced NF-kappaB activation preincubated for 15 mins followed by L18-MDP stimulation and further incubated for 8 hrs by SEAP reporter gene assay | B | 7.43 | pIC50 | 37 | nM | IC50 | Eur J Med Chem (2021) 215: 113252-113252 [PMID:33601309] |
| platelet derived growth factor receptor beta/platelet derived growth factor receptor alpha in Human [GtoPdb: 1804, 1803] [UniProtKB: P09619, P16234] | ||||||||
| 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: 1804, 1803] [UniProtKB: P05622, P26618] | ||||||||
| 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/Platelet-derived growth factor receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619] | ||||||||
| GtoPdb | - | - | 7.01 | pKi | 98.3 | nM | Ki | J Pharmacol Exp Ther (1997) 283: 1433-44 [PMID:9400019] |
| ChEMBL | Inhibition of PDGFR-beta (unknown origin) | B | 7 | pIC50 | <100 | nM | IC50 | J Med Chem (2020) 63: 14151-14183 [PMID:33135887] |
| 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] |
| checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757] | ||||||||
| ChEMBL | Inhibition of CHK1 (unknown origin) | B | 7.14 | pIC50 | 72 | nM | IC50 | Eur J Med Chem (2020) 203: 112524-112524 [PMID:32688199] |
| receptor interacting serine/threonine kinase 2/Serine/threonine-protein kinase RIPK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5014] [GtoPdb: 2190] [UniProtKB: O43353] | ||||||||
| ChEMBL | Inhibition of recombinant RIPK2 (unknown origin) using RS repeat peptide as substrate preincubated for 5 mins followed by substrate and ATP addition and further incubated for 2 hrs by ADP-Glo reagent based assay | B | 7.89 | pIC50 | 13 | nM | IC50 | Eur J Med Chem (2021) 215: 113252-113252 [PMID:33601309] |
| 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] |
| ChEMBL | Inhibition of full length WEE1 (unknown origin) assessed as reduction in cdc2/cyclin B phosphorylation using biotinylated histone H1 peptide (PKTPKKAKKL) preincubated for 30 mins followed by substrate and [gamma33P] addition and measured after 30 mins by scintillation proximity assay | B | 7.62 | pIC50 | 24 | nM | IC50 | J Med Chem (2020) 63: 14151-14183 [PMID:33135887] |
| ChEMBL | Inhibition of Wee1 (unknown origin) | B | 7.62 | pIC50 | 24 | nM | IC50 | Eur J Med Chem (2020) 203: 112524-112524 [PMID:32688199] |
| 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 | Inhibition of c-SRC (unknown origin) | B | 7 | pIC50 | <100 | nM | IC50 | J Med Chem (2020) 63: 14151-14183 [PMID:33135887] |
| 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 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]
