LY 294002 [Ligand Id: 6004] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL98350 (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] |
| 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 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 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 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 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 p110alpha by SPA assay | B | 6.2 | pIC50 | 630 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 2438-2442 [PMID:17339109] |
| 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 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) by fluorescent polarization assay | B | 6.26 | pIC50 | 550 | nM | IC50 | Medchemcomm (2012) 3: 1337-1355 |
| 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 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 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 by fluorescence polarization assay | B | 6.32 | pIC50 | 480 | nM | IC50 | Bioorg Med Chem (2019) 27: 2261-2267 [PMID:31029551] |
| 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 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 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 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) 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 PI3K beta (unknown origin) | B | 6.01 | pIC50 | 970 | nM | IC50 | J Med Chem (2020) 63: 14151-14183 [PMID:33135887] |
| 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 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 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 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 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 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
