LY 294002 [Ligand Id: 6004] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL98350 (Ly-294002, LY-294002) |
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| 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) | B | 6.01 | pIC50 | 970 | nM | IC50 | J Med Chem (2022) 65: 935-954 [PMID:33970631] |
| ChEMBL | Inhibition of human wild type PI3Kbeta expressed in Sf21 cells co-expressing N-terminal His-tagged human p85a using L-alpha-phosphatidylinositol substrate by TLC based phosphor imaging | B | 6.01 | pIC50 | 970 | nM | IC50 | Bioorg Med Chem (2012) 20: 3359-3367 [PMID:22520630] |
| ChEMBL | Inhibition of PI3K beta (unknown origin) | B | 6.01 | pIC50 | 970 | nM | IC50 | J Med Chem (2020) 63: 14151-14183 [PMID:33135887] |
| ChEMBL | Inhibition of PI3K beta (unknown origin) | B | 6.05 | pIC50 | 900 | nM | IC50 | J Med Chem (2022) 65: 893-921 [PMID:33539089] |
| ChEMBL | Inhibition of human recombinant PI3Kbeta expressed in baculovirus-infected Sf21 cells | B | 6.05 | pIC50 | 900 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5842-5847 [PMID:19748269] |
| ChEMBL | Inhibition of PI3K p110beta (unknown origin) | B | 6.13 | pIC50 | 736 | nM | IC50 | J Med Chem (2013) 56: 1922-1939 [PMID:23410005] |
| ChEMBL | Inhibition of immobilized N-LY294002 bead binding to PI3Kbeta (unknown origin) expressed in HEK293T cells incubated for 1 hr by LC-MS/MS analysis | B | 6.38 | pIC50 | 420 | nM | IC50 | Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261] |
| ChEMBL | Inhibition of GST-tagged human p110-beta expressed in SF9/Baculovirus system by SPA | B | 6.47 | pIC50 | 340 | nM | IC50 | Bioorg Med Chem (2007) 15: 5837-5844 [PMID:17601739] |
| ChEMBL | Inhibition of p110beta | B | 6.47 | pIC50 | 340 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 2438-2442 [PMID:17339109] |
| ChEMBL | Inhibition of GST-tagged human PI3K p110-beta by SPA | B | 6.47 | pIC50 | 340 | nM | IC50 | Bioorg Med Chem (2007) 15: 403-412 [PMID:17049248] |
| ChEMBL | Inhibition of PI3Kbeta using phosphatidylinositol as substrate by gamma33P[ATP] incorporation assay | B | 6.51 | pIC50 | 310 | nM | IC50 | J Med Chem (2012) 55: 8559-8581 [PMID:22924688] |
| ChEMBL | Inhibition of human PI3Kbeta | B | 6.51 | pIC50 | 306 | nM | IC50 | J Med Chem (2006) 49: 3857-3871 [PMID:16789742] |
| ChEMBL | Inhibition of PI-3K beta (unknown origin) | B | 6.57 | pIC50 | 270 | nM | IC50 | J Med Chem (2013) 56: 6386-6401 [PMID:23855836] |
| GtoPdb | - | - | 6.57 | pIC50 | 270 | nM | IC50 | J Med Chem (2013) 56: 6386-401 [PMID:23855836] |
| 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] | ||||||||
| GtoPdb | - | - | 6.15 | pKd | 710 | nM | Kd | ACS Chem Biol (2014) 9: 495-502 [PMID:24533473] |
| ChEMBL | Inhibition of PI3Kdelta (unknown origin) using PIP2 as substrate preincubated for 10 mins followed by substrate addition and measured after 1 hr by ELISA | B | 4.83 | pIC50 | 14900 | nM | IC50 | J Med Chem (2021) 64: 17468-17485 [PMID:34791873] |
| ChEMBL | Inhibition of PI3K p110delta (unknown origin) | B | 5.49 | pIC50 | 3223 | nM | IC50 | J Med Chem (2013) 56: 1922-1939 [PMID:23410005] |
| ChEMBL | Inhibition of PI3K p110delta (unknown origin) | B | 5.8 | pIC50 | 1600 | nM | IC50 | J Med Chem (2015) 58: 41-71 [PMID:25387153] |
| ChEMBL | Inhibition of immobilized N-LY294002 bead binding to PI3Kdelta (unknown origin) expressed in HEK293T cells incubated for 1 hr by LC-MS/MS analysis | B | 5.82 | pIC50 | 1530 | nM | IC50 | Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261] |
| ChEMBL | Inhibition of recombinant PI3Kdelta (unknown origin) using PI(3,4)P2 as substrate after 3 hrs incubation by competitive fluorescence polarization kinase activity assay | B | 5.87 | pIC50 | 1362 | nM | IC50 | Bioorg Med Chem (2015) 23: 1231-1240 [PMID:25693787] |
| ChEMBL | Inhibition of PI3Kdelta (unknown origin) using diC8-PI(4,5)P2 as substrate incubated for 3 hrs by fluorescence polarization assay | B | 5.87 | pIC50 | 1360 | nM | IC50 | Bioorg Med Chem (2019) 27: 2261-2267 [PMID:31029551] |
| ChEMBL | Inhibition of PI3Kdelta (unknown origin) using diC8-PI(4,5)P2 as substrate incubated for 3 hrs in presence of ATP by fluorescence polarization assay | B | 5.87 | pIC50 | 1360 | nM | IC50 | Eur J Med Chem (2019) 182: 111630-111630 [PMID:31446244] |
| ChEMBL | Inhibition of human PI3Kdelta | B | 5.88 | pIC50 | 1330 | nM | IC50 | J Med Chem (2006) 49: 3857-3871 [PMID:16789742] |
| ChEMBL | Inhibition of PI3Kdelta using phosphatidylinositol as substrate by gamma33P[ATP] incorporation assay | B | 5.98 | pIC50 | 1050 | nM | IC50 | J Med Chem (2012) 55: 8559-8581 [PMID:22924688] |
| ChEMBL | Inhibition of PI3Kdelta (unknown origin) incubated for 60 mins by kinase-glo luminescence assay | B | 6.02 | pIC50 | 950 | nM | IC50 | Eur J Med Chem (2016) 110: 326-339 [PMID:26854431] |
| ChEMBL | Inhibition of PI3Kdelta expressed in cells co-expressing N-terminal His-tagged human p85a using L-alpha-phosphatidylinositol substrate by TLC based phosphor imaging | B | 6.24 | pIC50 | 570 | nM | IC50 | Bioorg Med Chem (2012) 20: 3359-3367 [PMID:22520630] |
| ChEMBL | Inhibition of PI3K delta (unknown origin) | B | 6.24 | pIC50 | 570 | nM | IC50 | J Med Chem (2020) 63: 14151-14183 [PMID:33135887] |
| ChEMBL | Inhibition of PI3K delta (unknown origin) | B | 6.24 | pIC50 | 570 | nM | IC50 | J Med Chem (2022) 65: 893-921 [PMID:33539089] |
| ChEMBL | Inhibition of PI3Kdelta (unknown origin) | B | 6.24 | pIC50 | 570 | nM | IC50 | J Med Chem (2022) 65: 935-954 [PMID:33970631] |
| ChEMBL | Inhibition of recombinant PI3Kdelta 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 PI-3K delta (unknown origin) | B | 6.66 | pIC50 | 220 | nM | IC50 | J Med Chem (2013) 56: 6386-6401 [PMID:23855836] |
| GtoPdb | - | - | 6.66 | pIC50 | 220 | nM | IC50 | J Med Chem (2013) 56: 6386-401 [PMID:23855836] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/PI3-kinase p110-gamma subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736] | ||||||||
| ChEMBL | Inhibition of PI3K p110gamma (unknown origin) | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (2015) 58: 41-71 [PMID:25387153] |
| ChEMBL | Inhibition of PI3Kgamma (unknown origin) assessed as decrease in fluorescence intensity using phosphorylated substrate | B | 5.14 | pIC50 | 7260 | nM | IC50 | Eur J Med Chem (2014) 84: 454-465 [PMID:25050878] |
| ChEMBL | Inhibition of PI3Kgamma (unknown origin) using [33gammaP]ATP and phosphotidylinositol as substrate by scintillation proximity assay | B | 5.14 | pIC50 | 7260 | nM | IC50 | Med Chem Res (2013) 22: 5707-5716 |
| ChEMBL | Inhibition of human PI3Kgamma | B | 5.14 | pIC50 | 7260 | nM | IC50 | J Med Chem (2006) 49: 3857-3871 [PMID:16789742] |
| ChEMBL | Inhibition of PI3Kgamma (unknown origin) after 4 hrs | B | 5.14 | pIC50 | 7200 | nM | IC50 | Eur J Med Chem (2016) 108: 586-593 [PMID:26720154] |
| ChEMBL | Inhibition of PI3Kgamma using phosphatidylinositol as substrate by gamma33P[ATP] incorporation assay | B | 5.18 | pIC50 | 6600 | nM | IC50 | J Med Chem (2012) 55: 8559-8581 [PMID:22924688] |
| ChEMBL | Inhibition of PI-3K gamma (unknown origin) | B | 5.52 | pIC50 | 3020 | nM | IC50 | J Med Chem (2013) 56: 6386-6401 [PMID:23855836] |
| ChEMBL | Inhibition of PI3K p110gamma (unknown origin) | B | 5.75 | pIC50 | 1775 | nM | IC50 | J Med Chem (2013) 56: 1922-1939 [PMID:23410005] |
| ChEMBL | Inhibition of PI3Kgamma assessed as inhibition of 32P-PIP3 formation | B | 5.76 | pIC50 | 1720 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 756-760 [PMID:17095227] |
| ChEMBL | Inhibition of p110gamma | B | 5.8 | pIC50 | 1600 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 2438-2442 [PMID:17339109] |
| ChEMBL | Inhibition of His-tagged human p110gamma expressed in SF9/Baculovirus system by SPA | B | 5.8 | pIC50 | 1600 | nM | IC50 | Bioorg Med Chem (2007) 15: 5837-5844 [PMID:17601739] |
| ChEMBL | Inhibition of His-tagged PI3K p110gamma by SPA | B | 5.8 | pIC50 | 1600 | nM | IC50 | Bioorg Med Chem (2007) 15: 403-412 [PMID:17049248] |
| ChEMBL | Inhibition of PI3Kgamma (unknown origin) incubated for 60 mins by kinase-glo luminescence assay | B | 5.82 | pIC50 | 1500 | nM | IC50 | Eur J Med Chem (2016) 110: 326-339 [PMID:26854431] |
| GtoPdb | - | - | 5.92 | pIC50 | 1200 | nM | IC50 |
Bioorg Med Chem Lett (2009) 19: 2215-9 [PMID:19297156]; J Med Chem (2013) 56: 6386-401 [PMID:23855836] |
| ChEMBL | Inhibition of PI3Kgamma by luminescent kinase glo assay | B | 5.92 | pIC50 | 1200 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2215-2219 [PMID:19297156] |
| ChEMBL | Inhibition of PI3Kgamma (unknown origin) using diC8-PI(4,5)P2 as substrate incubated for 3 hrs in presence of ATP by fluorescence polarization assay | B | 6.02 | pIC50 | 950 | nM | IC50 | Eur J Med Chem (2019) 182: 111630-111630 [PMID:31446244] |
| ChEMBL | Inhibition of recombinant PI3Kgamma (unknown origin) using PI(3,4)P2 as substrate after 3 hrs incubation by competitive fluorescence polarization kinase activity assay | B | 6.02 | pIC50 | 947 | nM | IC50 | Bioorg Med Chem (2015) 23: 1231-1240 [PMID:25693787] |
| ChEMBL | Inhibition of PI3Kgamma (unknown origin) using diC8-PI(4,5)P2 as substrate incubated for 3 hrs by fluorescence polarization assay | B | 6.03 | pIC50 | 940 | nM | IC50 | Bioorg Med Chem (2019) 27: 2261-2267 [PMID:31029551] |
| phosphoinositide-3-kinase regulatory subunit 1/PI3-kinase p85-alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2506] [GtoPdb: 2503] [UniProtKB: P27986] | ||||||||
| ChEMBL | Inhibition of PI3K | B | 5.85 | pIC50 | 1400 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum NF54 | F | 5.52 | pIC50 | 3000 | nM | IC50 | J Med Chem (2018) 61: 8061-8077 [PMID:29771541] |
| ATM serine/threonine kinase/Serine-protein kinase ATM in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3797] [GtoPdb: 1934] [UniProtKB: Q13315] | ||||||||
| ChEMBL | Inhibition of ATM kinase using rabbit polyclonal antisera | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2005) 48: 569-585 [PMID:15658870] |
| ChEMBL | Inhibition of Mutated in ataxia telangiectasia protein ATM kinase | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 6083-6087 [PMID:15546735] |
| ChEMBL | Inhibition of ATM (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2013) 56: 6386-6401 [PMID:23855836] |
| ATR serine/threonine kinase/Serine-protein kinase ATR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5024] [GtoPdb: 1935] [UniProtKB: Q13535] | ||||||||
| ChEMBL | Inhibition of ATR kinase using rabbit polyclonal antisera | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2005) 48: 569-585 [PMID:15658870] |
| ChEMBL | Inhibition of Ataxia telangiectasia related protein ATR kinase | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 6083-6087 [PMID:15546735] |
| ChEMBL | Inhibition of ATR (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2013) 56: 6386-6401 [PMID:23855836] |
| mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345] | ||||||||
| ChEMBL | Inhibition of mTOR (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2019) 182: 111630-111630 [PMID:31446244] |
| ChEMBL | Inhibition of mTOR (unknown origin) after 40 mins by scintillation counting analysis | B | 5 | pIC50 | 9900 | nM | IC50 | Eur J Med Chem (2015) 102: 600-610 [PMID:26318067] |
| ChEMBL | Inhibition of MTOR | B | 5.17 | pIC50 | 6796 | nM | IC50 | Bioorg Med Chem (2011) 19: 6760-6767 [PMID:22014755] |
| ChEMBL | Inhibition of mTOR | B | 5.3 | pIC50 | 5000 | nM | IC50 | J Biol Chem (2007) 282: 24463-24470 [PMID:17562705] |
| ChEMBL | Inhibition of human mTOR by non-radiometric ADP-Glo assay | B | 5.41 | pIC50 | 3900 | nM | IC50 | ACS Med Chem Lett (2015) 6: 3-6 [PMID:25589915] |
| ChEMBL | inhibition of mTOR | B | 5.52 | pIC50 | 3018 | nM | IC50 | Bioorg Med Chem (2011) 19: 1915-1923 [PMID:21353571] |
| ChEMBL | Inhibition of mTOR (unknown origin) | B | 5.55 | pIC50 | 2800 | nM | IC50 | J Med Chem (2013) 56: 6386-6401 [PMID:23855836] |
| ChEMBL | Inhibition of mTOR protein isolated from HeLa cells | B | 5.6 | pIC50 | 2500 | nM | IC50 | J Med Chem (2005) 48: 569-585 [PMID:15658870] |
| ChEMBL | Inhibition of Mammalian target of Rapamycin mTOR | B | 5.6 | pIC50 | 2500 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 6083-6087 [PMID:15546735] |
| ChEMBL | Inhibition of mTOR (unknown origin) | B | 5.97 | pIC50 | 1060 | nM | IC50 | J Med Chem (2013) 56: 1922-1939 [PMID:23410005] |
| mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075134] [GtoPdb: 2109] [UniProtKB: P42346] | ||||||||
| ChEMBL | Inhibition of rat derived mTOR using [gamma32P]ATP | B | 5.6 | pIC50 | 2500 | nM | IC50 | J Med Chem (2015) 58: 41-71 [PMID:25387153] |
| Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309] | ||||||||
| ChEMBL | Inhibition of human recombinant Pim1 by ATP depletion assay | B | 5.4 | pIC50 | 4000 | nM | IC50 | J Med Chem (2009) 52: 74-86 [PMID:19072652] |
| ChEMBL | Inhibition of Pim1 | B | 5.4 | pIC50 | 4000 | nM | IC50 | J Med Chem (2009) 52: 1814-1827 [PMID:19256503] |
| ChEMBL | Inhibition of full length human Pim-2 kinase expressed in Escherichia coli BL21/DE3 using S6 peptide as substrate by coupled enzyme assay | B | 5.4 | pIC50 | 4000 | nM | IC50 | ACS Med Chem Lett (2021) 12: 1794-1801 [PMID:34795869] |
| ChEMBL | Inhibition of PIM1 in the presence of 20uM ATP | B | 6.09 | pIC50 | 820 | nM | IC50 | Biochem J (2007) 408: 297-315 [PMID:17850214] |
| Pim-3 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5407] [GtoPdb: 2160] [UniProtKB: Q86V86] | ||||||||
| ChEMBL | Inhibition of PIM3 in the presence of 20uM ATP | B | 5.85 | pIC50 | 1400 | nM | IC50 | Biochem J (2007) 408: 297-315 [PMID:17850214] |
| polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350] | ||||||||
| ChEMBL | Inhibition of AX-7503 binding to recombinant Plk1 by Western blot | B | 5.68 | pIC50 | 2100 | nM | IC50 | J Biol Chem (2007) 282: 2505-2511 [PMID:17135248] |
| ChEMBL | Inhibition of PLK1 in the presence of 5uM ATP | B | 5.7 | pIC50 | 2000 | nM | IC50 | Biochem J (2007) 408: 297-315 [PMID:17850214] |
| polo like kinase 3/Serine/threonine-protein kinase PLK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4897] [GtoPdb: 2170] [UniProtKB: Q9H4B4] | ||||||||
| ChEMBL | Inhibition of recombinant Plk3 assessed as casein substrate phosphorylation | B | 4.06 | pIC50 | 88000 | nM | IC50 | J Biol Chem (2007) 282: 2505-2511 [PMID:17135248] |
| ChEMBL | Inhibition of AX-7503 binding to recombinant Plk3 expressed in HeLa cells by Western blot | B | 5.52 | pIC50 | 3000 | nM | IC50 | J Biol Chem (2007) 282: 2505-2511 [PMID:17135248] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) | B | 6.1 | pKi | 799 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) | B | 5.55 | pIC50 | 2796 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 4.63 | pKi | 23359 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 4.44 | pIC50 | 36707 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) | B | 6.28 | pKi | 525 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) | B | 6 | pIC50 | 1002 | nM | IC50 | DrugMatrix in vitro pharmacology data |
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]
