BindingDB PrimarySearch

Found 11 Enz. Inhib. hit(s) for PDB: 2Y3A

Phosphatidylinositol 3-kinase regulatory subunit beta(Homo sapiens (Human))
Genentech

US Patent

BDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)

Ki: 70.2nMAssay Description:PI3K Binding assays are intended for determining the biochemical potency of small molecule PI3K inhibitors. The PI3K lipid kinase reaction is perform...More data for this Ligand-Target Pair

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3D Structure (crystal)

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
Genentech

Curated by ChEMBL

BDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)

IC50: 17nMAssay Description:Inhibition of GST-fused human recombinant PI3Kbeta expressed in baculovirus infected SF9 cells after 1 hr by scintillation proximity assay in presenc...More data for this Ligand-Target Pair

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3D Structure (crystal)

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
Genentech

Curated by ChEMBL

BDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)

IC50: 32nMAssay Description:Inhibition of recombinant PI3Kbeta assessed as PIP3 product formation by fluorescence polarization assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
Genentech

Curated by ChEMBL

BDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)

IC50: 33nMAssay Description:Inhibition of p110betaMore data for this Ligand-Target Pair

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3D Structure (crystal)

Phosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
Piramed Pharma

BDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)

IC50: 33nMpH: 7.5 T: 2°CAssay Description:Test compounds were added to reaction buffer containing yttrium silicate (Ysi) polylysine SPA beads (Amersham), and the enzyme was added to the assay...More data for this Ligand-Target Pair

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3D Structure (crystal)

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
Genentech

Curated by ChEMBL

BDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)

IC50: 33nMAssay Description:Inhibition of PI3Kbeta (unknown origin) using PIP2 as substrate after 1 hr by kinase-glo luminescence assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

Phosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
Piramed Pharma

BDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)

IC50: 54nMAssay Description:Inhibition of recombinant full length human N-terminal GST-tagged PI3K p110beta/untagged p85alpha expressed in baculovirus infected insect Sf9 cells ...More data for this Ligand-Target Pair

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3D Structure (crystal)

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
Genentech

Curated by ChEMBL

BDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)

IC50: 181nMAssay Description:Inhibition of PI3Kbeta (unknown origin) using PIP2:PS as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr in pr...More data for this Ligand-Target Pair

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3D Structure (crystal)

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
Genentech

Curated by ChEMBL

BDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)

IC50: 251nMAssay Description:Inhibition of PI3Kbeta (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins in pre...More data for this Ligand-Target Pair

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3D Structure (crystal)

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
Genentech

Curated by ChEMBL

BDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)

Kd: 16nMAssay Description:Binding constant for PIK3CB kinase domainMore data for this Ligand-Target Pair

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3D Structure (crystal)

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
Genentech

Curated by ChEMBL

BDBM25028(4-[2-(1H-indazol-4-yl)-6-[(4-methanesulfonylpipera...)

Kd: 2.10nMAssay Description:Binding affinity to human PI3Kbeta (P118 to S1070 residues) expressed in mammalian expression system by Kinomescan assayMore data for this Ligand-Target Pair

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3D Structure (crystal)

Filter my 11 hits

Targets 3▿
- Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform 8
- Phosphatidylinositol 3-kinase regulatory subunit alpha/4,5-bisphosphate 3-kinase catalytic subunit beta isoform 2
- Phosphatidylinositol 3-kinase regulatory subunit beta 1
Publications 11▿
- J Med Chem 51: 5522-32 (2008) 1
- J Med Chem 60: 1534-1554 (2017) 1
- Bioorg Med Chem Lett 23: 2606-13 (2013) 1
- Nat Chem Biol 6: 117-24 (2010) 1
- J Med Chem 60: 7524-7538 (2017) 1
- US Patent US10112932 (2018) 1
- Eur J Med Chem 136: 195-211 (2017) 1
- Eur J Med Chem 156: 831-846 (2018) 1
- J Med Chem 53: 1086-97 (2010) 1
- Nat Biotechnol 29: 1046-51 (2011) 1
- J Med Chem 60: 4023-4035 (2017) 1
Institutions 9▿
- Genentech 3
- Medical Research Council-Laboratory Of Molecular Biology 1
- Ambit Biosciences 1
- Hunan University Of Chinese Medicine 1
- West China Hospital Of Sichuan University 1
- Piramed Pharma 1
- University Of Basel 1
- Chinese Academy Of Sciences 1
- University Park Nottingham 1
Affinity: 2.1 to 2.5E+2 nM▿
- Ki 1
- IC50 8
- Kd 2
- Affinity ≤ nM
Xtal structures: 1
Docked structures: 0
Catalog Cmpds: 1