LY 294002 [Ligand Id: 6004] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL98350 (Ly-294002, LY-294002)
  • bromodomain containing 2/Bromodomain-containing protein 2 in Human [ChEMBL: CHEMBL1293289] [GtoPdb: 1944] [UniProtKB: P25440]
There should be some charts here, you may need to enable JavaScript!
  • bromodomain containing 3/Bromodomain-containing protein 3 in Human [ChEMBL: CHEMBL1795186] [GtoPdb: 2725] [UniProtKB: Q15059]
There should be some charts here, you may need to enable JavaScript!
  • bromodomain containing 4/Bromodomain-containing protein 4 in Human [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
There should be some charts here, you may need to enable JavaScript!
  • bromodomain testis associated/Bromodomain testis-specific protein in Human [ChEMBL: CHEMBL1795185] [GtoPdb: 2729] [UniProtKB: Q58F21]
There should be some charts here, you may need to enable JavaScript!
  • casein kinase 2, alpha prime polypeptide subunit/casein kinase 2, beta polypeptide subunit/casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II in Human [ChEMBL: CHEMBL2095191] [GtoPdb: 1550, 1551, 1549] [UniProtKB: P19784, P67870, P68400]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase in Human [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527]
There should be some charts here, you may need to enable JavaScript!
  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 beta/Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing beta polypeptide in Human [ChEMBL: CHEMBL5554] [GtoPdb: 2151] [UniProtKB: O00750]
There should be some charts here, you may need to enable JavaScript!
  • phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 alpha/Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing subunit alpha in Human [ChEMBL: CHEMBL1075102] [GtoPdb: 2150] [UniProtKB: O00443]
There should be some charts here, you may need to enable JavaScript!
  • phosphodiesterase 2A/Phosphodiesterase 2A in Human [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408]
There should be some charts here, you may need to enable JavaScript!
  • phosphodiesterase 5A/Phosphodiesterase 5A in Human [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074]
There should be some charts here, you may need to enable JavaScript!
  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha subunit in Human [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336]
  • PI3-kinase p110-alpha subunit in Bovine [ChEMBL: CHEMBL2498] [UniProtKB: P32871]
  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha subunit in Mouse [ChEMBL: CHEMBL2499] [GtoPdb: 2153] [UniProtKB: P42337]
There should be some charts here, you may need to enable JavaScript!
  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/PI3-kinase p110-beta subunit in Human [ChEMBL: CHEMBL3145] [GtoPdb: 2154] [UniProtKB: P42338]
There should be some charts here, you may need to enable JavaScript!
  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/PI3-kinase p110-delta subunit in Human [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329]
There should be some charts here, you may need to enable JavaScript!
  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/PI3-kinase p110-gamma subunit in Human [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736]
There should be some charts here, you may need to enable JavaScript!
  • phosphoinositide-3-kinase regulatory subunit 1/PI3-kinase p85-alpha subunit in Human [ChEMBL: CHEMBL2506] [GtoPdb: 2503] [UniProtKB: P27986]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • ATM serine/threonine kinase/Serine-protein kinase ATM in Human [ChEMBL: CHEMBL3797] [GtoPdb: 1934] [UniProtKB: Q13315]
There should be some charts here, you may need to enable JavaScript!
  • ATR serine/threonine kinase/Serine-protein kinase ATR in Human [ChEMBL: CHEMBL5024] [GtoPdb: 1935] [UniProtKB: Q13535]
There should be some charts here, you may need to enable JavaScript!
  • mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345]
  • mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Rat [ChEMBL: CHEMBL1075134] [GtoPdb: 2109] [UniProtKB: P42346]
There should be some charts here, you may need to enable JavaScript!
  • Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309]
There should be some charts here, you may need to enable JavaScript!
  • Pim-3 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM3 in Human [ChEMBL: CHEMBL5407] [GtoPdb: 2160] [UniProtKB: Q86V86]
There should be some charts here, you may need to enable JavaScript!
  • polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350]
There should be some charts here, you may need to enable JavaScript!
  • polo like kinase 3/Serine/threonine-protein kinase PLK3 in Human [ChEMBL: CHEMBL4897] [GtoPdb: 2170] [UniProtKB: Q9H4B4]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
bromodomain containing 2/Bromodomain-containing protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293289] [GtoPdb: 1944] [UniProtKB: P25440]
GtoPdb - - 5.85 pKd 1410 nM Kd ACS Chem Biol (2014) 9: 495-502 [PMID:24533473]
ChEMBL Inhibition of immobilized N-LY294002 bead binding to BRD2 (unknown origin) expressed in HEK293T cell nuclear extract incubated for 1 hr by LC-MS/MS analysis B 4.99 pIC50 10300 nM IC50 Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261]
bromodomain containing 3/Bromodomain-containing protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795186] [GtoPdb: 2725] [UniProtKB: Q15059]
GtoPdb - - 6.03 pKd 930 nM Kd ACS Chem Biol (2014) 9: 495-502 [PMID:24533473]
ChEMBL Inhibition of immobilized N-LY294002 bead binding to BRD3 (unknown origin) expressed in HEK293T cell nuclear extract incubated for 1 hr by LC-MS/MS analysis B 4.86 pIC50 13700 nM IC50 Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261]
bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
GtoPdb - - 5.74 pKd 1830 nM Kd ACS Chem Biol (2014) 9: 495-502 [PMID:24533473]
ChEMBL Inhibition of immobilized N-LY294002 bead binding to C-terminal Flag-tagged BRD4 (unknown origin) expressed in HEK293T cell nuclear extract incubated for 1 hr by LC-MS/MS analysis B 4.91 pIC50 12400 nM IC50 Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261]
bromodomain testis associated/Bromodomain testis-specific protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795185] [GtoPdb: 2729] [UniProtKB: Q58F21]
ChEMBL Inhibition of human recombinant BRDT B 4.91 pIC50 12430 nM IC50 J Med Chem (2016) 59: 9305-9320 [PMID:27559828]
casein kinase 2, alpha prime polypeptide subunit/casein kinase 2, beta polypeptide subunit/casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2095191] [GtoPdb: 1550, 1551, 1549] [UniProtKB: P19784, P67870, P68400]
ChEMBL Inhibition of His-tagged human CK2 expressed in Sf9 cells B 5.16 pIC50 6900 nM IC50 Biochem J (2000) 351: 95-105 [PMID:10998351]
CYP1A2/Cytochrome P450 1A2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3356] [GtoPdb: 1319] [UniProtKB: P05177]
ChEMBL DRUGMATRIX: CYP450, 1A2 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) B 6 pIC50 1000 nM IC50 DrugMatrix in vitro pharmacology data
protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527]
ChEMBL Affinity for DNA-dependent protein kinase(DNA-PK) from HeLa cell extract B 5.22 pKi 6000 nM Ki Bioorg Med Chem Lett (2003) 13: 3083-3086 [PMID:12941339]
ChEMBL Competitive inhibition of DNA-PK B 5.22 pKi 6000 nM Ki Bioorg Med Chem Lett (2012) 22: 5352-5359 [PMID:22835870]
ChEMBL Competitive inhibition of DNA-PK (unknown origin) in the presence of ATP B 5.22 pKi 6000 nM Ki J Med Chem (2013) 56: 6386-6401 [PMID:23855836]
ChEMBL Inhibition of DNA-dependent protein kinase B 5.8 pIC50 1600 nM IC50 Bioorg Med Chem Lett (2008) 18: 4885-4890 [PMID:18678488]
ChEMBL Inhibition of DNA-dependent protein kinase B 5.8 pIC50 1600 nM IC50 Bioorg Med Chem Lett (2010) 20: 3649-3653 [PMID:20472428]
ChEMBL Inhibition of DNA dependent protein kinase isolated from HeLa cells B 5.82 pIC50 1500 nM IC50 J Med Chem (2005) 48: 569-585 [PMID:15658870]
ChEMBL Inhibitory activity against DNA-dependent protein kinase receptor B 5.83 pIC50 1470 nM IC50 J Med Chem (2005) 48: 7829-7846 [PMID:16302822]
ChEMBL Inhibition of DNA dependent protein kinase isolated from HeLa cells B 5.83 pIC50 1470 nM IC50 J Med Chem (2005) 48: 569-585 [PMID:15658870]
ChEMBL In vitro inhibition of DNA-dependent protein kinase(DNA-PK) from HeLa (human carcinoma) cells. B 5.85 pIC50 1400 nM IC50 Bioorg Med Chem Lett (2003) 13: 3083-3086 [PMID:12941339]
ChEMBL Inhibition of DNA-dependent protein kinase (DNA-PK) of HeLa cell nuclear cell extract B 5.85 pIC50 1400 nM IC50 Bioorg Med Chem Lett (2001) 11: 2837-2841 [PMID:11597411]
ChEMBL Inhibition of DNA-PK (unknown origin) B 5.85 pIC50 1400 nM IC50 J Med Chem (2013) 56: 6386-6401 [PMID:23855836]
ChEMBL Inhibition of DNA-PK B 5.89 pIC50 1300 nM IC50 Bioorg Med Chem Lett (2011) 21: 966-970 [PMID:21216595]
ChEMBL Inhibition of DNA-PK purified from human HeLa nuclear extracts B 5.92 pIC50 1200 nM IC50 J Med Chem (2015) 58: 41-71 [PMID:25387153]
ChEMBL Inhibitory activity against DNA-dependent protein kinase (DNA-PK) B 5.92 pIC50 1200 nM IC50 Bioorg Med Chem Lett (2004) 14: 6083-6087 [PMID:15546735]
ChEMBL Inhibition of human DNA-PK using EPPLSQEAFADLWKK as substrate by HTRF assay B 6.52 pIC50 300 nM IC50 Eur J Med Chem (2016) 110: 326-339 [PMID:26854431]
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
ChEMBL Inhibition of GSK3-beta in human U87MG cells by ELISA B 5.09 pIC50 8100 nM IC50 J Med Chem (2008) 51: 2147-2157 [PMID:18345609]
L-type calcium channel alpha 1C/beta 2A in Rabbit (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3638171] [UniProtKB: P15381, P54288]
ChEMBL Inhibition of Cav1.2 calcium current measured using whole cell patch clamp in human HEK293 cells transfected with rabbit L-type calcium channel subunits F 4.92 pIC50 12000 nM IC50 IC50 data for the L-type calcium channel extracted from a set of literature articles
phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 beta/Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing beta polypeptide in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5554] [GtoPdb: 2151] [UniProtKB: O00750]
ChEMBL Inhibition of human PI3KC2beta by non-radiometric ADP-Glo assay B 4.98 pIC50 10400 nM IC50 ACS Med Chem Lett (2015) 6: 3-6 [PMID:25589915]
ChEMBL Inhibition of Glu-tagged PI3K C2-beta by SPA B 5.68 pIC50 2100 nM IC50 Bioorg Med Chem (2007) 15: 403-412 [PMID:17049248]
ChEMBL Inhibition of glu-tagged PI3K C2-beta expressed in SF9/Baculovirus system by SPA B 5.68 pIC50 2100 nM IC50 Bioorg Med Chem (2007) 15: 5837-5844 [PMID:17601739]
ChEMBL Inhibition of PI3Kc2beta B 5.68 pIC50 2100 nM IC50 Bioorg Med Chem Lett (2007) 17: 2438-2442 [PMID:17339109]
phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 alpha/Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075102] [GtoPdb: 2150] [UniProtKB: O00443]
ChEMBL Inhibition of human PI3KC2alpha by non-radiometric ADP-Glo assay B 4.57 pIC50 27000 nM IC50 ACS Med Chem Lett (2015) 6: 3-6 [PMID:25589915]
phosphodiesterase 2A/Phosphodiesterase 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408]
ChEMBL Inhibition of human platelet phosphodiesterase 2 B 4.4 pIC50 40000 nM IC50 Bioorg Med Chem Lett (2004) 14: 2847-2851 [PMID:15125945]
phosphodiesterase 5A/Phosphodiesterase 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074]
ChEMBL DRUGMATRIX: Phosphodiesterase PDE5 enzyme inhibition (substrate: [3H]cGMP + cGMP) B 5.02 pIC50 9614 nM IC50 DrugMatrix in vitro pharmacology data
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336]
ChEMBL Binding affinity for PI3-kinase isolated from HeLa cells; Range is 20-120 B 5.22 pKi 6000 nM Ki J Med Chem (2005) 48: 569-585 [PMID:15658870]
ChEMBL Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate preincubated for 10 mins followed by substrate addition and measured after 1 hr by ELISA B 4.2 pIC50 62800 nM IC50 J Med Chem (2021) 64: 17468-17485 [PMID:34791873]
ChEMBL Inhibition of human PI3Kalpha by ELISA B 5.21 pIC50 6180 nM IC50 Bioorg Med Chem (2021) 31: 115976-115976 [PMID:33388654]
ChEMBL Inhibition of PI3Kalpha (unknown origin) incubated for 60 mins by kinase-glo luminescence assay B 5.4 pIC50 4000 nM IC50 Eur J Med Chem (2016) 110: 326-339 [PMID:26854431]
ChEMBL Inhibition of immobilized N-LY294002 bead binding to PI3Kalpha (unknown origin) expressed in HEK293T cells incubated for 1 hr by LC-MS/MS analysis B 5.63 pIC50 2370 nM IC50 Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261]
ChEMBL Inhibition of Phosphatidylinositol 3-kinase p110 alpha subunit B 5.64 pIC50 2300 nM IC50 Bioorg Med Chem Lett (2004) 14: 6083-6087 [PMID:15546735]
ChEMBL Inhibition of human recombinant p110 alpha Phosphatidylinositol 3-kinase B 5.64 pIC50 2300 nM IC50 J Med Chem (2005) 48: 569-585 [PMID:15658870]
ChEMBL Inhibition of PI3Kalpha using phosphatidylinositol as substrate by gamma33P[ATP] incorporation assay B 6.14 pIC50 730 nM IC50 J Med Chem (2012) 55: 8559-8581 [PMID:22924688]
ChEMBL Inhibition of human PI3Kalpha B 6.14 pIC50 720 nM IC50 J Med Chem (2006) 49: 3857-3871 [PMID:16789742]
ChEMBL Inhibition of p110alpha by SPA assay B 6.2 pIC50 630 nM IC50 Bioorg Med Chem Lett (2007) 17: 2438-2442 [PMID:17339109]
ChEMBL Inhibition of PI3Kalpha using diC8-PI(4,5)P2 as substrate after 3 hrs by competitive fluorescence polarization assay B 6.2 pIC50 630 nM IC50 Bioorg Med Chem (2012) 20: 2837-2844 [PMID:22480851]
ChEMBL Inhibition of human PI3KCalpha by non-radiometric ADP-Glo assay B 6.22 pIC50 600 nM IC50 ACS Med Chem Lett (2015) 6: 3-6 [PMID:25589915]
ChEMBL Inhibition of human PI3Kalpha expressed in Sf9 cells by fluorescent polarization assay B 6.26 pIC50 550 nM IC50 J Med Chem (2010) 53: 8523-8533 [PMID:21121631]
ChEMBL Inhibition of PI3Kalpha (unknown origin) by fluorescent polarization assay B 6.26 pIC50 550 nM IC50 Medchemcomm (2012) 3: 1337-1355
ChEMBL Inhibition of PI3K p110alpha (unknown origin) B 6.26 pIC50 550 nM IC50 J Med Chem (2015) 58: 41-71 [PMID:25387153]
ChEMBL Inhibition of PI3Kalpha (unknown origin) B 6.3 pIC50 500 nM IC50 J Med Chem (2022) 65: 935-954 [PMID:33970631]
ChEMBL Inhibition of PI3Kalpha after 80 mins B 6.3 pIC50 500 nM IC50 Bioorg Med Chem Lett (2011) 21: 966-970 [PMID:21216595]
ChEMBL Inhibition of PI3K alpha (unknown origin) B 6.3 pIC50 500 nM IC50 J Med Chem (2020) 63: 14151-14183 [PMID:33135887]
ChEMBL Inhibition of PI3K alpha (unknown origin) B 6.3 pIC50 500 nM IC50 J Med Chem (2022) 65: 893-921 [PMID:33539089]
ChEMBL Inhibition of recombinant PI3Kalpha (unknown origin) using PI(3,4)P2 as substrate after 3 hrs incubation by competitive fluorescence polarization kinase activity assay B 6.32 pIC50 481 nM IC50 Bioorg Med Chem (2015) 23: 1231-1240 [PMID:25693787]
ChEMBL Inhibition of PI3Kalpha (unknown origin) using diC8-PI(4,5)P2 as substrate incubated for 3 hrs in presence of ATP by fluorescence polarization assay B 6.32 pIC50 480 nM IC50 Eur J Med Chem (2019) 182: 111630-111630 [PMID:31446244]
ChEMBL Inhibition of PI3Kalpha (unknown origin) using diC8-PI(4,5)P2 as substrate incubated for 3 hrs by fluorescence polarization assay B 6.32 pIC50 480 nM IC50 Bioorg Med Chem (2019) 27: 2261-2267 [PMID:31029551]
ChEMBL Inhibition of PI3K p110alpha (unknown origin) B 6.45 pIC50 356 nM IC50 J Med Chem (2013) 56: 1922-1939 [PMID:23410005]
ChEMBL Inhibition of PI-3K alpha (unknown origin) B 6.52 pIC50 300 nM IC50 J Med Chem (2013) 56: 6386-6401 [PMID:23855836]
ChEMBL Inhibition of PI3Kalpha by luminescent kinase glo assay B 6.7 pIC50 200 nM IC50 Bioorg Med Chem Lett (2009) 19: 2215-2219 [PMID:19297156]
GtoPdb - - 6.7 pIC50 200 nM IC50 Bioorg Med Chem Lett (2009) 19: 2215-9 [PMID:19297156];
J Med Chem (2013) 56: 6386-401 [PMID:23855836]
PI3-kinase p110-alpha subunit in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2498] [UniProtKB: P32871]
ChEMBL Inhibition of His-tagged bovine PI3K expressed in Sf9 cells B 5 pIC50 10000 nM IC50 Biochem J (2000) 351: 95-105 [PMID:10998351]
ChEMBL Inhibition of bovine brain PI3Kalpha in presence of [p32-gamma]-ATP measured after 10 mins by liquid scintillation spectroscopy B 5.2 pIC50 6300 nM IC50 J Med Chem (2022) 65: 16033-16061 [PMID:36503229]
ChEMBL Inhibition of GST-tagged bovine PI3K p110-alpha by SPA B 6.2 pIC50 630 nM IC50 Bioorg Med Chem (2007) 15: 403-412 [PMID:17049248]
ChEMBL Inhibition of GST-tagged bovine p110-alpha expressed in SF9/Baculovirus system by SPA B 6.2 pIC50 630 nM IC50 Bioorg Med Chem (2007) 15: 5837-5844 [PMID:17601739]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha subunit in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2499] [GtoPdb: 2153] [UniProtKB: P42337]
ChEMBL Inhibition of mouse recombinant PI3Kalpha expressed in baculovirus-infected Sf21 cells B 6.3 pIC50 500 nM IC50 Bioorg Med Chem Lett (2009) 19: 5842-5847 [PMID:19748269]
ChEMBL Inhibition of mouse wild type PI3Kalpha expressed in Sf21 cells co-expressing N-terminal His-tagged human p85a using L-alpha-phosphatidylinositol substrate by TLC based phosphor imaging B 6.3 pIC50 500 nM IC50 Bioorg Med Chem (2012) 20: 3359-3367 [PMID:22520630]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/PI3-kinase p110-beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3145] [GtoPdb: 2154] [UniProtKB: P42338]
GtoPdb - - 6.57 pKd 270 nM Kd ACS Chem Biol (2014) 9: 495-502 [PMID:24533473]
ChEMBL Inhibition of PI3K p110beta (unknown origin) B 4.8 pIC50 16000 nM IC50 J Med Chem (2015) 58: 41-71 [PMID:25387153]
ChEMBL Inhibition of PI3Kbeta (unknown origin) using PIP2 as substrate preincubated for 10 mins followed by substrate addition and measured after 1 hr by ELISA B 4.88 pIC50 13100 nM IC50 J Med Chem (2021) 64: 17468-17485 [PMID:34791873]
ChEMBL Inhibition of PI3Kbeta (unknown origin) incubated for 60 mins by kinase-glo luminescence assay B 5.52 pIC50 3000 nM IC50 Eur J Med Chem (2016) 110: 326-339 [PMID:26854431]
ChEMBL Inhibition of recombinant PI3Kbeta (unknown origin) using PI(3,4)P2 as substrate after 3 hrs incubation by competitive fluorescence polarization kinase activity assay B 6.01 pIC50 983 nM IC50 Bioorg Med Chem (2015) 23: 1231-1240 [PMID:25693787]
ChEMBL Inhibition of PI3Kbeta (unknown origin) using diC8-PI(4,5)P2 as substrate incubated for 3 hrs in presence of ATP by fluorescence polarization assay B 6.01 pIC50 980 nM IC50 Eur J Med Chem (2019) 182: 111630-111630 [PMID:31446244]
ChEMBL Inhibition of PI3Kbeta (unknown origin) using diC8-PI(4,5)P2 as substrate incubated for 3 hrs by fluorescence polarization assay B 6.01 pIC50 980 nM IC50 Bioorg Med Chem (2019) 27: 2261-2267 [PMID:31029551]
ChEMBL Inhibition of PI3Kbeta (unknown origin)