palbociclib [Ligand Id: 7380] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL189963 (Ibrance, Palbociclib, PD-0332991)
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  • cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493]
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  • cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
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  • cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802]
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  • cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535]
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  • cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535Q15078]
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  • cyclin dependent kinase 6/Cyclin-dependent kinase 6 in Human [ChEMBL: CHEMBL2508] [GtoPdb: 1978] [UniProtKB: Q00534]
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  • cyclin dependent kinase 7/Cyclin-dependent kinase 7 in Human [ChEMBL: CHEMBL3055] [GtoPdb: 1979] [UniProtKB: P50613]
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  • cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750]
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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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  • colony stimulating factor 1 receptor/Macrophage colony stimulating factor receptor in Human [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333]
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  • NUAK family kinase 1/NUAK family SNF1-like kinase 1 in Human [ChEMBL: CHEMBL5784] [GtoPdb: 2129] [UniProtKB: O60285]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/PI3-kinase p110-delta subunit in Human [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329]
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  • platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619]
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  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
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  • FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
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  • Janus kinase 3/Tyrosine-protein kinase JAK3 in Human [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
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  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
cyclin dependent kinase 2/CDK2/Cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038469] [GtoPdb: 1973] [UniProtKB: P20248P24941]
ChEMBL Inhibition of CDK2/cyclin A (unknown origin) in presence of [gamma-33P]-ATP by KINOMEscan assay B 5.3 pKi >5000 nM Ki J Med Chem (2017) 60: 1892-1915 [PMID:28156111]
ChEMBL Inhibition of CDK2/cyclin A (unknown origin) expressed in baculovirus infected insect cells using GST-tagged pRB (792 to 928 residues) as substrate preincubated for 2 mins followed by [gamma32P]ATP addition measured after 15 mins by beta counting method B 5 pIC50 >10000 nM IC50 J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
ChEMBL Inhibition of CDK2/cyclinA (unknown origin) B 6.64 pIC50 230 nM IC50 J. Med. Chem. (2014) 57: 578-599 [PMID:24417566]
cyclin dependent kinase 6/CDK6/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111455] [GtoPdb: 1978] [UniProtKB: P24385Q00534]
GtoPdb - - 7.44 pIC50 36 nM IC50 WO2014183520A1. Thiophene miazines derivate, preparation method therefor, and medical application thereof (2014)
GtoPdb - - 7.8 pIC50 16 nM IC50 Mol. Cancer Ther. (2004) 3: 1427-38 [PMID:15542782]
ChEMBL Inhibition of CDK6/cyclinD1 (unknown origin) B 8.42 pIC50 3.76 nM IC50 J. Med. Chem. (2014) 57: 578-599 [PMID:24417566]
cyclin dependent kinase 6/CDK6/cyclin D2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3301386] [GtoPdb: 1978] [UniProtKB: P30279Q00534]
GtoPdb - - 7.44 pIC50 36 nM IC50 WO2014183520A1. Thiophene miazines derivate, preparation method therefor, and medical application thereof (2014)
GtoPdb - - 7.8 pIC50 16 nM IC50 Mol. Cancer Ther. (2004) 3: 1427-38 [PMID:15542782]
ChEMBL Inhibition of CDK6/cyclin D2 (unknown origin) expressed in baculovirus infected insect cells using GST-tagged pRB (792 to 928 residues) as substrate preincubated for 2 mins followed by [gamma32P]ATP addition measured after 15 mins by beta counting method B 7.82 pIC50 15 nM IC50 J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
ChEMBL Inhibition of CDK6/cyclin D2 (unknown origin) expressed in baculovirus infected insect cells using GST-fused pRb (792 to 928) as substrate preincubated for 2 mins followed by [gamma-32P]-ATP addition measured after 15 mins by beta plate counting analysis B 8.05 pIC50 9 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 3420-3435 [PMID:26115571]
cyclin dependent kinase 6/CDK6/cyclin D3 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111448] [GtoPdb: 1978] [UniProtKB: P30281Q00534]
ChEMBL Inhibition of CDK6/cyclin D3 (unknown origin) in presence of [gamma-33P]-ATP by KINOMEscan assay B 7.57 pKi 27 nM Ki J Med Chem (2017) 60: 1892-1915 [PMID:28156111]
GtoPdb - - 7.44 pIC50 36 nM IC50 WO2014183520A1. Thiophene miazines derivate, preparation method therefor, and medical application thereof (2014)
ChEMBL Inhibition of CDK6/Cyclin-D3 (unknown origin) using histoneH1 as substrate after 90 mins by ADP-Glo assay B 7.72 pIC50 19 nM IC50 Eur J Med Chem (2018) 144: 1-28 [PMID:29247857]
GtoPdb - - 7.8 pIC50 16 nM IC50 Mol. Cancer Ther. (2004) 3: 1427-38 [PMID:15542782]
cyclin dependent kinase 9/CDK9/cyclin T1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111389] [GtoPdb: 1981] [UniProtKB: O60563P50750]
ChEMBL Inhibition of CDK9/cyclin T1 (unknown origin) in presence of [gamma-33P]-ATP by KINOMEscan assay B 6.44 pKi 364 nM Ki J Med Chem (2017) 60: 1892-1915 [PMID:28156111]
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 5 pIC50 >10000 nM IC50 Eur. J. Med. Chem. (2016) 110: 291-301 [PMID:26851505]
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493P14635]
ChEMBL Inhibition of CDK1/cyclin B (unknown origin) in presence of [gamma-33P]-ATP by KINOMEscan assay B 5.3 pKi >5000 nM Ki J Med Chem (2017) 60: 1892-1915 [PMID:28156111]
ChEMBL Inhibition of CDK1/cyclin B (unknown origin) expressed in baculovirus infected insect cells using GST-tagged pRB (792 to 928 residues) as substrate preincubated for 2 mins followed by [gamma32P]ATP addition measured after 15 mins by beta counting method B 5 pIC50 >10000 nM IC50 J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL Inhibition of CDK2 (unknown origin) expressed in baculovirus infected insect cells using GST-fused pRb (792 to 928) as substrate preincubated for 2 mins followed by [gamma-32P]-ATP addition measured after 15 mins by beta plate counting analysis B 5.3 pIC50 >5000 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 3420-3435 [PMID:26115571]
ChEMBL Caliper Assay: Selected compounds disclosed herein were tested in CDK4/cyclinD1, CDK6/CycD3 CDK2/CycA and CDK2/cyclinE kinase assays by Nanosyn (Santa Clara, Calif.) to determine their inhibitory effect on these CDKs. The assays were performed using microfluidic kinase detection technology (Caliper Assay Platform). The compounds were tested in 12-point dose-response format in singlicate at Km for ATP. Phosphoacceptor substrate peptide concentration used was 1 μM for all assays and Staurosporine was used as the reference compound for all assays. Specifics of each assay are as described below:CDK2/CyclinA: Enzyme concentration: 0.2 nM; ATP concentration: 50 μM; Incubation time: 3 hr.CDK2/CyclinE: Enzyme concentration: 0.28 nM; ATP concentration: 100 μM; Incubation time: 1 hr.CDK4/CyclinD1: Enzyme concentration: 1 nM; ATP concentration: 200 μM; Incubation time: 10 hr.CDK6/CyclinD3: Enzyme concentration: 1 nM; ATP concentration: 300 μM; Incubation time: 3 hr. B 8 pIC50 10 nM IC50 US-9464092-B2. Transient protection of normal cells during chemotherapy (2016)
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094128] [GtoPdb: 1973] [UniProtKB: P20248P24941P78396]
ChEMBL Inhibition of Cyclin dependent kinase 2-cyclin A B 5.3 pIC50 >5000 nM IC50 J. Med. Chem. (2005) 48: 2388-2406 [PMID:15801831]
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864P24941]
ChEMBL Inhibition of CDK2/Cyclin E (unknown origin) expressed in sf9 cells using histone H1 as substrate in presence of [gamma33P]-ATP B 5.04 pIC50 9200 nM IC50 Eur. J. Med. Chem. (2016) 110: 291-301 [PMID:26851505]
cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802]
GtoPdb - - 7.36 pIC50 44 nM IC50 WO2014183520A1. Thiophene miazines derivate, preparation method therefor, and medical application thereof (2014)
ChEMBL Inhibition of CDK4 B 7.7 pIC50 <20 nM IC50 Eur. J. Med. Chem. (2010) 45: 727-737 [PMID:19954867]
ChEMBL Inhibition of CDK4 (unknown origin) using histone H1 as substrate after 10 mins in presence of [gamma32P]ATP B 7.74 pIC50 18 nM IC50 Eur J Med Chem (2016) 122: 546-556 [PMID:27448913]
ChEMBL Inhibition of CDK4 (unknown origin) B 7.8 pIC50 16 nM IC50 Eur. J. Med. Chem. (2016) 110: 291-301 [PMID:26851505]
ChEMBL Inhibition of CDK4 B 7.96 pIC50 11 nM IC50 J. Med. Chem. (2010) 53: 6779-6810 [PMID:20925433]
ChEMBL Inhibition of CDK4 in human MOLM13 cells assessed as inhibition of Rb phosphorylation at Ser780 after 24 hrs B 7.96 pIC50 11 nM IC50 J. Med. Chem. (2014) 57: 3430-3449 [PMID:24641103]
ChEMBL Inhibition of CDK4 (unknown origin) B 7.96 pIC50 11 nM IC50 Eur J Med Chem (2017) 142: 424-458 [PMID:28911822]
GtoPdb - - 7.96 pIC50 11 nM IC50 Mol. Cancer Ther. (2004) 3: 1427-38 [PMID:15542782]
cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095942] [GtoPdb: 1976] [UniProtKB: P11802P24385P30279P30281]
GtoPdb - - 7.36 pIC50 44 nM IC50 WO2014183520A1. Thiophene miazines derivate, preparation method therefor, and medical application thereof (2014)
ChEMBL Inhibition of Cyclin-dependent kinase 4-cyclinD B 7.96 pIC50 11 nM IC50 J. Med. Chem. (2005) 48: 2388-2406 [PMID:15801831]
GtoPdb - - 7.96 pIC50 11 nM IC50 Mol. Cancer Ther. (2004) 3: 1427-38 [PMID:15542782]
cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907601] [GtoPdb: 1976] [UniProtKB: P11802P24385]
ChEMBL Inhibition of CDK4/cyclin D1 (unknown origin) in presence of [gamma-33P]-ATP by KINOMEscan assay B 8.52 pKi 3 nM Ki J Med Chem (2017) 60: 1892-1915 [PMID:28156111]
GtoPdb - - 7.36 pIC50 44 nM IC50 WO2014183520A1. Thiophene miazines derivate, preparation method therefor, and medical application thereof (2014)
ChEMBL Inhibition of CDK4/cyclinD1 (unknown origin) B 7.96 pIC50 11 nM IC50 J. Med. Chem. (2014) 57: 578-599 [PMID:24417566]
ChEMBL Inhibition of CDK4/cyclin D1 (unknown origin) expressed in baculovirus infected insect cells using GST-fused pRb (792 to 928) as substrate preincubated for 2 mins followed by [gamma-32P]-ATP addition measured after 15 mins by beta plate counting analysis B 7.96 pIC50 11 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 3420-3435 [PMID:26115571]
ChEMBL Inhibition of CDK4/cyclin D1 (unknown origin) expressed in baculovirus infected insect cells using GST-tagged pRB (792 to 928 residues) as substrate preincubated for 2 mins followed by [gamma32P]ATP addition measured after 15 mins by beta counting method B 7.96 pIC50 11 nM IC50 J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
GtoPdb - - 7.96 pIC50 11 nM IC50 Mol. Cancer Ther. (2004) 3: 1427-38 [PMID:15542782]
ChEMBL Caliper Assay: Selected compounds disclosed herein were tested in CDK4/cyclinD1, CDK6/CycD3 CDK2/CycA and CDK2/cyclinE kinase assays by Nanosyn (Santa Clara, Calif.) to determine their inhibitory effect on these CDKs. The assays were performed using microfluidic kinase detection technology (Caliper Assay Platform). The compounds were tested in 12-point dose-response format in singlicate at Km for ATP. Phosphoacceptor substrate peptide concentration used was 1 μM for all assays and Staurosporine was used as the reference compound for all assays. Specifics of each assay are as described below:CDK2/CyclinA: Enzyme concentration: 0.2 nM; ATP concentration: 50 μM; Incubation time: 3 hr.CDK2/CyclinE: Enzyme concentration: 0.28 nM; ATP concentration: 100 μM; Incubation time: 1 hr.CDK4/CyclinD1: Enzyme concentration: 1 nM; ATP concentration: 200 μM; Incubation time: 10 hr.CDK6/CyclinD3: Enzyme concentration: 1 nM; ATP concentration: 300 μM; Incubation time: 3 hr. B 8 pIC50 10 nM IC50 US-9464092-B2. Transient protection of normal cells during chemotherapy (2016)
ChEMBL Inhibition of CDK4/cyclinD1 (unknown origin) using retinoblastoma as substrate after 30 mins by autoradiography in presence of [gamma-32P]ATP B 8.27 pIC50 5.36 nM IC50 J. Med. Chem. (2014) 57: 578-599 [PMID:24417566]
ChEMBL Inhibition of CDK4/cyclin D1 (unknown origin) using Rb as substrate after 60 mins by scintillation counting analysis in presence of [r-33P]ATP B 8.7 pIC50 2 nM IC50 J. Med. Chem. (2014) 57: 3430-3449 [PMID:24641103]
cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535]
ChEMBL Inhibition of CDK5 (unknown origin) using histone H1 as substrate in presence of [gamma33P]-ATP B 5 pIC50 >10000 nM IC50 Eur. J. Med. Chem. (2016) 110: 291-301 [PMID:26851505]
cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535Q15078]
ChEMBL Inhibition of CDK5/p25 (unknown origin) expressed in baculovirus infected insect cells using GST-tagged pRB (792 to 928 residues) as substrate preincubated for 2 mins followed by [gamma32P]ATP addition measured after 15 mins by beta counting method B 5 pIC50 >10000 nM IC50 J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
cyclin dependent kinase 6/Cyclin-dependent kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2508] [GtoPdb: 1978] [UniProtKB: Q00534]
GtoPdb - - 7.44 pIC50 36 nM IC50 WO2014183520A1. Thiophene miazines derivate, preparation method therefor, and medical application thereof (2014)
ChEMBL Inhibition of CDK6 (unknown origin) using histone H1 as substrate after 10 mins in presence of [gamma32P]ATP B 7.68 pIC50 21 nM IC50 Eur J Med Chem (2016) 122: 546-556 [PMID:27448913]
ChEMBL Inhibition of CDK6 B 7.8 pIC50 16 nM IC50 J. Med. Chem. (2010) 53: 6779-6810 [PMID:20925433]
ChEMBL Inhibition of CDK6 (unknown origin) B 7.8 pIC50 16 nM IC50 Eur J Med Chem (2017) 142: 424-458 [PMID:28911822]
GtoPdb - - 7.8 pIC50 16 nM IC50 Mol. Cancer Ther. (2004) 3: 1427-38 [PMID:15542782]
cyclin dependent kinase 7/Cyclin-dependent kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3055] [GtoPdb: 1979] [UniProtKB: P50613]
ChEMBL Inhibition of CDK7 (unknown origin) B 5 pIC50 >10000 nM IC50 Eur. J. Med. Chem. (2016) 110: 291-301 [PMID:26851505]
cyclin dependent kinase 7/Cyclin-dependent kinase 7/ cyclin H in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111288] [GtoPdb: 1979] [UniProtKB: P50613P51946]
ChEMBL Inhibition of CDK7/cyclin H (unknown origin) in presence of [gamma-33P]-ATP by KINOMEscan assay B 5.3 pKi >5000 nM Ki J Med Chem (2017) 60: 1892-1915 [PMID:28156111]
cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750]
ChEMBL Inhibition of CDK9 (unknown origin) B 6.05 pIC50 892 nM IC50 Eur. J. Med. Chem. (2016) 110: 291-301 [PMID:26851505]
ChEMBL Inhibition of CDK9 (unknown origin) B 6.1 pIC50 794.33 nM IC50 J. Med. Chem. (2013) 56: 6991-7002 [PMID:23937569]
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. (2014) 57: 578-599 [PMID:24417566]
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 FMS (unknown origin) B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2014) 57: 578-599 [PMID:24417566]
NUAK family kinase 1/NUAK family SNF1-like kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5784] [GtoPdb: 2129] [UniProtKB: O60285]
ChEMBL Inhibition of ARK5 (unknown origin) B 5.3 pIC50 >5000 nM IC50 J. Med. Chem. (2014) 57: 578-599 [PMID:24417566]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/PI3-kinase p110-delta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329]
ChEMBL Inhibition of PI3Kdelta (unknown origin) B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2014) 57: 578-599 [PMID:24417566]
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. (2014) 57: 578-599 [PMID:24417566]
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. (2014) 57: 578-599 [PMID:24417566]
FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
ChEMBL Inhibition of FYN (unknown origin) B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2014) 57: 578-599 [PMID:24417566]
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
ChEMBL Inhibition of JAK3 (unknown origin) B 7.2 pIC50 63.1 nM IC50 J. Med. Chem. (2013) 56: 6991-7002 [PMID:23937569]
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. (2014) 57: 578-599 [PMID:24417566]
ChEMBL Inhibition of GST-fused human FLT3 cytoplasmic domain (amino acids 564 to 993) using Ulight-JAK1 as substrate after 1 hr by TR-FRET assay B 5.46 pIC50 3480 nM IC50 J. Med. Chem. (2014) 57: 3430-3449 [PMID:24641103]
ChEMBL Inhibition of FLT3 ITD mutant in human MOLM13 cells assessed as inhibition of STAT5 phosphorylation at Tyr694 after 24 hrs B 5.52 pIC50 >3000 nM IC50 J. Med. Chem. (2014) 57: 3430-3449 [PMID:24641103]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]