PF-543 [Ligand Id: 6623] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3134157 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| EPH receptor A2/Ephrin type-A receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317] | ||||||||
| ChEMBL | Inhibition of EPHA2 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 7697-7716 [PMID:35439002] |
| EPH receptor B2/Ephrin type-B receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323] | ||||||||
| ChEMBL | Inhibition of EPHB2 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 7697-7716 [PMID:35439002] |
| epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
| ChEMBL | Inhibition of EGFR (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 7697-7716 [PMID:35439002] |
| fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362] | ||||||||
| ChEMBL | Inhibition of FGFR1 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 7697-7716 [PMID:35439002] |
| fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802] | ||||||||
| ChEMBL | Inhibition of FGFR2 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 7697-7716 [PMID:35439002] |
| fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607] | ||||||||
| ChEMBL | Inhibition of FGFR3 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 7697-7716 [PMID:35439002] |
| fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3973] [GtoPdb: 1811] [UniProtKB: P22455] | ||||||||
| ChEMBL | Inhibition of FGFR4 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 7697-7716 [PMID:35439002] |
| Insulin-like growth factor I receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069] | ||||||||
| ChEMBL | Inhibition of IGF1R (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 7697-7716 [PMID:35439002] |
| Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213] | ||||||||
| ChEMBL | Inhibition of Insulin receptor (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 7697-7716 [PMID:35439002] |
| colony stimulating factor 1 receptor/Macrophage colony stimulating factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333] | ||||||||
| ChEMBL | Inhibition of CSF1R (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 7697-7716 [PMID:35439002] |
| 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 | Inhibition of PDGFRalpha (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 7697-7716 [PMID:35439002] |
| platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619] | ||||||||
| ChEMBL | Inhibition of PDGFRbeta (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 7697-7716 [PMID:35439002] |
| erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626] | ||||||||
| ChEMBL | Inhibition of ERBB2 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 7697-7716 [PMID:35439002] |
| erb-b2 receptor tyrosine kinase 4/Receptor protein-tyrosine kinase erbB-4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3009] [GtoPdb: 1799] [UniProtKB: Q15303] | ||||||||
| ChEMBL | Inhibition of ERBB4 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 7697-7716 [PMID:35439002] |
| sphingosine kinase 1/Sphingosine kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4394] [GtoPdb: 2204] [UniProtKB: Q9NYA1] | ||||||||
| ChEMBL | Binding affinity to SK1 (unknown origin) assessed as inhibition of sphingosine phosphorylation | B | 8.3 | pKd | 5 | nM | Kd | J Med Chem (2018) 61: 9811-9840 [PMID:29969256] |
| ChEMBL | Inhibition of His6 tagged human SphK1 expressed in Sf21 cells using FITC-sphingosine as substrate preincubated for 90 mins prior substrate addition by Caliper assay | B | 8.37 | pKi | 4.3 | nM | Ki | ACS Med Chem Lett (2014) 5: 1329-1333 [PMID:25516793] |
| ChEMBL | Inhibition of SK1 (unknown origin) | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (2016) 59: 965-984 [PMID:26780304] |
| GtoPdb | - | - | 8.44 | pKi | 3.6 | nM | Ki | Biochem J (2012) 444: 79-88 [PMID:22397330] |
| ChEMBL | Inhibition of recombinant human C-terminal His-tagged SPHK1 expressed in fall armyworm sf21 cells using sphingosine as substrate after 1 hr by FITC-based caliper assay | B | 8.44 | pKi | 3.6 | nM | Ki | J Med Chem (2017) 60: 3933-3957 [PMID:28406646] |
| ChEMBL | Inhibition of human C-terminal His6-tagged SphK1 expressed in baculovirus infected Sf21 insect cells | B | 8.44 | pKi | 3.6 | nM | Ki | Eur J Med Chem (2017) 139: 461-481 [PMID:28822281] |
| ChEMBL | Inhibition of recombinant human SphK1 expressed in baculovirus infected Sf9 cells assessed as decrease in [33P]SIP production using D-erythro-sphingosine as substrate in presence of [gamma33P]-ATP by scintillation counting method | B | 8.44 | pKi | 3.6 | nM | Ki | Bioorg Med Chem (2021) 30: 115941-115941 [PMID:33385956] |
| ChEMBL | Competitive inhibition of recombinant human C-terminal His-tagged SphK1 expressed in baculovirus infected Sf21 cells using varying concentrations of FITC-sphingosine as substrate incubated for 30 mins by LC-MS/MS analysis | B | 8.44 | pKi | 3.6 | nM | Ki | Eur J Med Chem (2020) 206: 112713-112713 [PMID:32919113] |
| ChEMBL | Competitive-inhibition of recombinant human C-terminal His6-tagged Sphk1 expressed in baculovirus infected Sf21 insect cells using varying levels of sphingosine as substrate measured after 30 mins by LC-MS analysis | B | 8.44 | pKi | 3.6 | nM | Ki | Eur J Med Chem (2021) 212: 113121-113121 [PMID:33445156] |
| ChEMBL | Inhibition of human recombinant SphK1 expressed in Sf9 cells assessed as radiolabeled products using 5 uM sphingosine and 10 uM gamma[32P]ATP by liquid scintillation counting | B | 8.44 | pKi | 3.6 | nM | Ki | J Med Chem (2015) 58: 1879-1899 [PMID:25643074] |
| ChEMBL | Inhibition of recombinant His-tagged human SK1 assessed as production of [32P]-S1P using 10 uM sphingosine as substrate by TLC method in presence of 100 uM [gamma32P]-ATP | B | 6.41 | pIC50 | 387 | nM | IC50 | J Med Chem (2016) 59: 965-984 [PMID:26780304] |
| ChEMBL | Inhibition of SphK1 (unknown origin) using D-Sph as substrate incubated for 40 mins by ADP-Glo Plus luminescence kinase assay | B | 6.97 | pIC50 | 107 | nM | IC50 | Bioorg Med Chem (2023) 93: 117441-117441 [PMID:37586181] |
| ChEMBL | Inhibition of SphK1 (unknown origin) | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem Lett (2021) 34: 127754-127754 [PMID:33347967] |
| ChEMBL | Inhibition of recombinant SK1 (unknown origin) using sphingosine and [gamma-32P]ATP as substrate after 30 mins | B | 7.55 | pIC50 | 28 | nM | IC50 | Medchemcomm (2013) 4: 1394-1399 [PMID:24396570] |
| ChEMBL | Inhibition of SK1 (unknown origin) using 5 uM of sphingosine as substrate | B | 7.55 | pIC50 | 28 | nM | IC50 | J Med Chem (2016) 59: 965-984 [PMID:26780304] |
| ChEMBL | Inhibition of GFP-tagged SK1 (unknown origin) expressed in HEK293 cells using Sph as substrate measured after 30 mins in presence of [gamma32P]ATP by Cerenkov counting analysis | B | 7.55 | pIC50 | 28 | nM | IC50 | J Med Chem (2019) 62: 3658-3676 [PMID:30889352] |
| ChEMBL | Inhibition of SPHK1 in human whole-blood using C17-sphingosine as substrate assessed as reduction in C17-S1P production preincubated for 30 mins followed by substrate addition measured after 10 mins by MS analysis | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2017) 60: 2562-2572 [PMID:28231433] |
| ChEMBL | Inhibition of C-terminal His6-tagged human SPHK1 expressed in baculovirus infected Sf21 insect cells using FITC-sphingosine as substrate preincubated for 90 mins followed by substrate addition in presence of ATP by caliper mobility shift assay | B | 8.44 | pIC50 | 3.6 | nM | IC50 | J Med Chem (2022) 65: 7697-7716 [PMID:35439002] |
| ChEMBL | Inhibition of SK1 (unknown origin) using 3 uM of sphingosine as substrate | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2016) 59: 965-984 [PMID:26780304] |
| ChEMBL | Inhibition of recombinant human C-terminus His-tagged SphK1 expressed in baculovirus infected Sf21 cells using FITC-sphingosine as substrate preincubated for 90 mins followed by substrate addition in presence of ATP by caliper fluorescent assay | B | 8.57 | pIC50 | 2.7 | nM | IC50 | Eur J Med Chem (2021) 213: 113164-113164 [PMID:33454547] |
| ChEMBL | Inhibition of human C-terminal His6-tagged SPHK1 expressed in fall armyworm sf9 cells assessed as reduction in S1P formation using sphingosine as substrate after 1 hr by FITC-based caliper assay | B | 8.57 | pIC50 | 2.7 | nM | IC50 | J Med Chem (2017) 60: 2562-2572 [PMID:28231433] |
| ChEMBL | Inhibition of recombinant C-terminal His6-tagged human SphK1 expressed in baculovirus infected sf21 cells using FITC-sphingosine as substrate after 1 hr in presence of ATP by microfluidic capillary electrophoresis mobility shift assay | B | 8.57 | pIC50 | 2.7 | nM | IC50 | Bioorg Med Chem (2017) 25: 3046-3052 [PMID:28408190] |
| GtoPdb | - | - | 8.57 | pIC50 | 2.7 | nM | IC50 | J Med Chem (2017) 60: 2562-2572 [PMID:28231433] |
| ChEMBL | Inhibition of SPHK1 (unknown origin) using sphingosine-fluorescein as substrate incubated for 1 hr in presence of ATP by mobility shift assay | B | 8.59 | pIC50 | 2.6 | nM | IC50 | J Med Chem (2022) 65: 7697-7716 [PMID:35439002] |
| ChEMBL | Inhibition of human C-terminal His6-tagged SPHK1 expressed in fall armyworm sf9 cells assessed as reduction in ADP formation using sphingosine as substrate preincubated for 15 mins followed by substrate addition after 1 hr by transcreener-based fluorescence polarization assay | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2017) 60: 2562-2572 [PMID:28231433] |
| GtoPdb | - | - | 8.7 | pIC50 | 2 | nM | IC50 | Biochem J (2012) 444: 79-88 [PMID:22397330] |
| ChEMBL | Inhibition of SPHK1 in human MDA1483 cells using C17-sphingosine as substrate assessed as reduction in C17-S1P formation preincubated for 30 mins with substrate measured after 15 mins by LC-MS analysis | B | 9.1 | pIC50 | 0.8 | nM | IC50 | J Med Chem (2017) 60: 2562-2572 [PMID:28231433] |
| sphingosine kinase 1/Sphingosine kinase 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2401605] [GtoPdb: 2204] [UniProtKB: Q8CI15] | ||||||||
| ChEMBL | Inhibition of SphK1 in mouse erythrocytes using sphingosine as substrate by luminescence assay | B | 8.44 | pKi | 3.6 | nM | Ki | ACS Med Chem Lett (2016) 7: 229-234 [PMID:26985306] |
| sphingosine kinase 2/Sphingosine kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3023] [GtoPdb: 2205] [UniProtKB: Q9NRA0] | ||||||||
| ChEMBL | Inhibition of SK2 (unknown origin) | B | 8.44 | pKi | 3.6 | nM | Ki | J Med Chem (2019) 62: 3658-3676 [PMID:30889352] |
| ChEMBL | Inhibition of recombinant human SK2 assessed as production of [32P] S1P using 10 uM sphingosine as substrate by TLC method in presence of 100 uM [gamma32P]-ATP relative to control | B | 4.77 | pIC50 | 17000 | nM | IC50 | J Med Chem (2016) 59: 965-984 [PMID:26780304] |
| ChEMBL | Inhibition of SK2 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 965-984 [PMID:26780304] |
| ChEMBL | Inhibition of SPHK2 (unknown origin) using sphingosine-fluorescein as substrate incubated for 1 hr in presence of ATP by mobility shift assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 7697-7716 [PMID:35439002] |
| ChEMBL | Inhibition of SphK2 (unknown origin) | B | 5.27 | pIC50 | 5400 | nM | IC50 | Bioorg Med Chem Lett (2021) 34: 127754-127754 [PMID:33347967] |
| ChEMBL | Inhibition of recombinant human full-length N-terminal His-tagged SK2 expressed in baculovirus infected Sf9 insect cells using Sph as substrate measured after 30 mins in presence of [gamma32P]ATP by Cerenkov counting analysis | B | 5.3 | pIC50 | >5000 | nM | IC50 | J Med Chem (2019) 62: 3658-3676 [PMID:30889352] |
| ChEMBL | Inhibition of SPHK2 (unknown origin) | B | 5.3 | pIC50 | >5000 | nM | IC50 | J Med Chem (2022) 65: 7697-7716 [PMID:35439002] |
| ChEMBL | Inhibition of SphK2 (unknown origin) using NBD-Sph as substrate by fluorescent plate reader analysis | B | 6.32 | pIC50 | 480 | nM | IC50 | Bioorg Med Chem (2023) 93: 117441-117441 [PMID:37586181] |
| ChEMBL | Inhibition of human recombinant C-terminal His6 tagged SphK2 expressed in baculovirus infected sf21 cells using FITC-sphingosine as substrate after 1 hr in presence of ATP by microfluidic capillary electrophoresis mobility shift assay | B | 6.44 | pIC50 | 360 | nM | IC50 | Bioorg Med Chem (2017) 25: 3046-3052 [PMID:28408190] |
| ChEMBL | Inhibition of SPHK2 (unknown origin) by FITC-based caliper assay | B | 6.45 | pIC50 | 356 | nM | IC50 | J Med Chem (2017) 60: 2562-2572 [PMID:28231433] |
| ChEMBL | Inhibition of recombinant human C-terminus His-tagged SphK2 expressed in baculovirus infected Sf21 cells using FITC-sphingosine as substrate preincubated for 90 mins followed by substrate addition in presence of ATP by caliper fluorescent assay | B | 6.45 | pIC50 | 356 | nM | IC50 | Eur J Med Chem (2021) 213: 113164-113164 [PMID:33454547] |
| GtoPdb | - | - | 6.45 | pIC50 | 356 | nM | IC50 | J Med Chem (2017) 60: 2562-2572 [PMID:28231433] |
| tyrosine kinase non receptor 2/Tyrosine kinase non-receptor protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4599] [GtoPdb: 2246] [UniProtKB: Q07912] | ||||||||
| ChEMBL | Inhibition of ACK1 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 7697-7716 [PMID:35439002] |
| 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 ABL (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 7697-7716 [PMID:35439002] |
| Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187] | ||||||||
| ChEMBL | Inhibition of BTK (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 7697-7716 [PMID:35439002] |
| 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 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 7697-7716 [PMID:35439002] |
| ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949] | ||||||||
| ChEMBL | Inhibition of RET (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 7697-7716 [PMID:35439002] |
| 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 SRC (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 7697-7716 [PMID:35439002] |
| 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 VEGFR1 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 7697-7716 [PMID:35439002] |
| kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] | ||||||||
| ChEMBL | Inhibition of VEGFR2 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 7697-7716 [PMID:35439002] |
| fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916] | ||||||||
| ChEMBL | Inhibition of VEGFR3 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 7697-7716 [PMID:35439002] |
ChEMBL data shown on this page come from version 35:
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]
