BDBM185147 (Z)-but-2-enedioic acid;8-(6-methoxypyridin-3-yl)-3-methyl-1-[4-piperazin-1-yl-3-(trifluoromethyl)phenyl]imidazo[4,5-c]quinolin-2-one::BGT-226::US9284315, BGT-226

SMILES COc1ccc(cn1)-c1ccc2ncc3n(C)c(=O)n(-c4ccc(N5CCNCC5)c(c4)C(F)(F)F)c3c2c1

InChI Key InChIKey=BMMXYEBLEBULND-UHFFFAOYSA-N

Data  8 IC50  1 Kd

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 18 hits for monomerid = 185147   

TargetSerine/threonine-protein kinase mTOR(Human)
Zuanzhu Pharma

US Patent
LigandPNGBDBM185147(BGT-226 | (Z)-but-2-enedioic acid;8-(6-methoxypyri...)
Affinity DataIC50: 1.99nMpH: 7.5 T: 2°CAssay Description:1. Preparation of test reagents {circle around (1)} 1x kinase buffer (50 mM HEPES, pH 7.5, 10 mM MgCl2, 1 mM EGTA, 3 mM MnCl, 0.01% Tween-20, 2 mM DT...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/21/2017
Entry Details
US Patent

TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Human)
Bioland Laboratory (Guangzhou Regenerative Medicine and Health - Guangdong Laboratory)

Curated by ChEMBL
LigandPNGBDBM185147(BGT-226 | (Z)-but-2-enedioic acid;8-(6-methoxypyri...)
Affinity DataIC50: 4nMAssay Description:Inhibition of PI3Kalpha (unknown origin) expressed in baculovirus expression system using L-alpha-phosphatidylinositol as substrate by luminescence a...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/21/2023
Entry Details
PubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Human)
Bioland Laboratory (Guangzhou Regenerative Medicine and Health - Guangdong Laboratory)

Curated by ChEMBL
LigandPNGBDBM185147(BGT-226 | (Z)-but-2-enedioic acid;8-(6-methoxypyri...)
Affinity DataEC50:  4nMAssay Description:Inhibition of PI3K alpha (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Human)
Bioland Laboratory (Guangzhou Regenerative Medicine and Health - Guangdong Laboratory)

Curated by ChEMBL
LigandPNGBDBM185147(BGT-226 | (Z)-but-2-enedioic acid;8-(6-methoxypyri...)
Affinity DataIC50: 4nMAssay Description:Inhibition of PI3Kalpha (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Human)
Bioland Laboratory (Guangzhou Regenerative Medicine and Health - Guangdong Laboratory)

Curated by ChEMBL
LigandPNGBDBM185147(BGT-226 | (Z)-but-2-enedioic acid;8-(6-methoxypyri...)
Affinity DataIC50: 4nMAssay Description:Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate measured after 30 mins by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetPhosphatidylinositol 3-kinase catalytic subunit type 3(Human)
Georgetown University

Curated by ChEMBL
LigandPNGBDBM185147(BGT-226 | (Z)-but-2-enedioic acid;8-(6-methoxypyri...)
Affinity DataEC50:  7nMAssay Description:Inhibition of human VPS34 assessed as reduction in PIP3 product complex formation measured after 30 mins in presence of ATP by quantitative PI3P ELIS...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Human)
Bioland Laboratory (Guangzhou Regenerative Medicine and Health - Guangdong Laboratory)

Curated by ChEMBL
LigandPNGBDBM185147(BGT-226 | (Z)-but-2-enedioic acid;8-(6-methoxypyri...)
Affinity DataIC50: 38nMAssay Description:Inhibition of PI3Kdelta (unknown origin) expressed in baculovirus expression system using L-alpha-phosphatidylinositol as substrate by luminescence a...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/21/2023
Entry Details
PubMed
LigandPNGBDBM185147(BGT-226 | (Z)-but-2-enedioic acid;8-(6-methoxypyri...)
Affinity DataIC50: 38nMAssay Description:Inhibition of PI3Kgamma (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMed
LigandPNGBDBM185147(BGT-226 | (Z)-but-2-enedioic acid;8-(6-methoxypyri...)
Affinity DataIC50: 38nMAssay Description:Inhibition of PI3Kgamma (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured for 1 hr in presenc...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
LigandPNGBDBM185147(BGT-226 | (Z)-but-2-enedioic acid;8-(6-methoxypyri...)
Affinity DataEC50:  38nMAssay Description:Inhibition of PI3K gamma (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Human)
Bioland Laboratory (Guangzhou Regenerative Medicine and Health - Guangdong Laboratory)

Curated by ChEMBL
LigandPNGBDBM185147(BGT-226 | (Z)-but-2-enedioic acid;8-(6-methoxypyri...)
Affinity DataIC50: 41.9nMpH: 7.5 T: 2°CAssay Description:1. Preparation of test reagents{circle around (1)} 1x kinase buffer (50 mM HEPES, pH 7.5, 3 mM MgCl2, 1 mM EGTA, 100 mM NaCl, 0.03% CHAPS, 2 mM DTT);...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/21/2017
Entry Details
US Patent

LigandPNGBDBM185147(BGT-226 | (Z)-but-2-enedioic acid;8-(6-methoxypyri...)
Affinity DataEC50:  56nMAssay Description:Inhibition of human PI3Kbeta assessed as reduction in PIP3 product complex formation measured after 30 mins in presence of ATP by quantitative PI3P E...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
LigandPNGBDBM185147(BGT-226 | (Z)-but-2-enedioic acid;8-(6-methoxypyri...)
Affinity DataIC50: 63nMAssay Description:Inhibition of PI3Kbeta (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured for 1 hr in presence...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
LigandPNGBDBM185147(BGT-226 | (Z)-but-2-enedioic acid;8-(6-methoxypyri...)
Affinity DataEC50:  63nMAssay Description:Inhibition of PI3K beta (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
LigandPNGBDBM185147(BGT-226 | (Z)-but-2-enedioic acid;8-(6-methoxypyri...)
Affinity DataIC50: 63nMAssay Description:Inhibition of PI3Kbeta (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMed
LigandPNGBDBM185147(BGT-226 | (Z)-but-2-enedioic acid;8-(6-methoxypyri...)
Affinity DataEC50:  63nMAssay Description:Inhibition of human PI3Kbeta assessed as reduction in PIP3 product complex formationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
LigandPNGBDBM185147(BGT-226 | (Z)-but-2-enedioic acid;8-(6-methoxypyri...)
Affinity DataIC50: 63nMAssay Description:Inhibition of PI3Kbeta (unknown origin) expressed in baculovirus expression system using L-alpha-phosphatidylinositol as substrate by luminescence as...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/21/2023
Entry Details
PubMed
TargetFerrochelatase, mitochondrial [R115L](Human)
Technical University of Munich

LigandPNGBDBM185147(BGT-226 | (Z)-but-2-enedioic acid;8-(6-methoxypyri...)
Affinity DataKd:  3.40E+3nMAssay Description:Briefly, 5 mg of a protein mixture of the four cell lines or a single cell line were incubated with compound dilution series in DMSO (3 nM, 10 nM, 30...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/30/2016
Entry Details Article
PubMed