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Target Snapshot

CHEMBL4005 Target Snapshot

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform · SINGLE PROTEIN · Homo sapiens

10,597Compounds
1,726Assays
15Approved Drugs
12,529.0Activities
Free Research Context

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Broader Open DB context

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As of 2026-09-13

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform shows approved-linked disease relevance led by neoplasm. 5 more disease programs remain visible in the same review block. 7 linked drugs keep the current disease frame grounded. Protein identity stays anchored to UniProt P42336. Start with neoplasm, then reuse UniProt P42336 as the stable protein anchor across project notes and exports.

Review focus
Review-ready target frame

Start with neoplasm, then reuse UniProt P42336 as the stable protein anchor across project notes and exports.

ChEMBL component mapping + Open Targets-ready proxy + ChEMBL 36 via Core Engine 2026-09-13 7 linked drugs
Open source guide
Disease program
neoplasm

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform shows approved-linked disease relevance led by neoplasm. 5 more disease programs remain visible in the same review block. 7 linked drugs remain visible in the same block.

Start review with neoplasm because it currently carries approved-linked support. Linked drugs include ALPELISIB, BAY-1082439, COPANLISIB, COPANLISIB HYDROCHLORIDE. This disease block keeps the Open Targets-ready contract explicit while current evidence comes from ChEMBL mechanism and indication mappings.

Disease source · ChEMBL drug mechanism + indication proxy
Approved-linked Open Targets-ready proxy 7 linked drugs
Open disease block
Protein anchor
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform

Review this target as Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform, mapped to UniProt P42336. Sequence length is 1068 aa.

Protein source · UniProt accession via ChEMBL component mapping
UniProt P42336 Protein 1068 aa
Open protein block
Identity Layer

Cross-source identity

Keep the review anchor, source IDs, and context contract aligned before reusing this target elsewhere.

This review treats Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform as ChEMBL target CHEMBL4005, mapped to UniProt P42336. Disease framing currently uses the Open Targets-ready proxy contract.

Review anchor
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
SINGLE PROTEIN · Homo sapiens
As of 2026-09-13
ChEMBL target ID
CHEMBL4005
Primary anchor for compounds, assays, approvals, and exports
ChEMBL 36 via Core Engine As of 2026-09-13
www.ebi.ac.uk
UniProt accession
P42336
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
UniProt accession via ChEMBL component mapping As of 2026-09-13
www.uniprot.org
Disease evidence contract
Open Targets-ready proxy
ChEMBL drug mechanism + indication proxy
ChEMBL drug mechanism + indication proxy As of 2026-09-13
www.ebi.ac.uk

Reuse the same identifiers in notes, watch rules, exports, and review packs so provenance stays stable across surfaces.

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UniProt Target Context
UniProt accession via ChEMBL component mapping

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Disease Relevance & Evidence Level
ChEMBL drug mechanism + indication proxy

Use this block first when you need to confirm why neoplasm is currently framed as approved-linked support. It currently carries 7 linked drugs in the same disease frame.

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Evidence Card
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Overview

Basic Information

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UniProt Context

UniProt Target Context

Reviewable protein naming and mapping context for this target snapshot.

Protein LabelPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
UniProt AccessionP42336
Component TypeProtein
Sequence Length1068 aa

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform

Source · UniProt accession via ChEMBL component mapping
Review Cue

How to read this target

Review this target as Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform, mapped to UniProt P42336. Sequence length is 1068 aa.

Mapped IDP42336
Review namePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
OrganismHomo sapiens
Disease Relevance

Disease Relevance & Evidence Level

Open Targets-ready disease context using the current target-indication evidence contract.

Approved-linked Open Targets-ready proxy

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform shows approved-linked disease relevance led by neoplasm. 5 more disease programs remain visible in the same review block.

Approved-linked Approved
neoplasm
7 linked drugs · 7 direct · 7 efficacy
Linked drugALPELISIB
Linked drugBAY-1082439
Linked drugCOPANLISIB
Linked drugCOPANLISIB HYDROCHLORIDE
Approved-linked Approved
breast cancer
4 linked drugs · 4 direct · 4 efficacy
Linked drugALPELISIB
Linked drugCOPANLISIB
Linked drugCOPANLISIB HYDROCHLORIDE
Linked drugINAVOLISIB
Approved-linked Approved
breast carcinoma
3 linked drugs · 3 direct · 3 efficacy
Linked drugALPELISIB
Linked drugCOPANLISIB
Linked drugCOPANLISIB HYDROCHLORIDE
Approved-linked Approved
cancer
3 linked drugs · 3 direct · 3 efficacy
Linked drugALPELISIB
Linked drugINAVOLISIB
Linked drugSERABELISIB
Approved-linked Approved
breast neoplasm
2 linked drugs · 2 direct · 2 efficacy
Linked drugALPELISIB
Linked drugINAVOLISIB
Approved-linked Approved
follicular lymphoma
2 linked drugs · 2 direct · 2 efficacy
Linked drugCOPANLISIB
Linked drugCOPANLISIB HYDROCHLORIDE
Source · ChEMBL drug mechanism + indication proxy
Review Cue

How to read disease relevance

Start review with neoplasm because it currently carries approved-linked support. Linked drugs include ALPELISIB, BAY-1082439, COPANLISIB, COPANLISIB HYDROCHLORIDE. This disease block keeps the Open Targets-ready contract explicit while current evidence comes from ChEMBL mechanism and indication mappings.

Lead diseaseneoplasm
Strongest levelApproved-linked
Block modeOpen Targets-ready proxy
Clinical Profile

Clinical Phase Distribution

15
Approved
13
Phase III
48
Phase II
11
Phase I
Assay Mix

Activity Type Distribution

IC509,899.0
KI1,530.0
EC50122.0
KD978.0
Lead Set

Top Inhibitors (by pChEMBL)

ChEMBL IDpChEMBLTypeValue (nM)Phase
CHEMBL3770993 10.8 Ki 0.016 Preclinical
CHEMBL1236962 10.72 Ki 0.019 Clinical
CHEMBL1236962 10.72 IC50 0.019 Clinical
CHEMBL5953956 10.68 Ki 0.021 Preclinical
CHEMBL5778370 10.66 Ki 0.022 Preclinical
CHEMBL6019298 10.64 Ki 0.023 Preclinical
CHEMBL5750027 10.62 Ki 0.024 Preclinical
CHEMBL5867381 10.62 Ki 0.024 Preclinical
CHEMBL5208487 10.59 Ki 0.026 Preclinical
CHEMBL5855663 10.59 Ki 0.026 Preclinical
Distribution

pChEMBL Value Distribution

658
5.0
1400
5.5
1525
6.0
1357
6.5
1415
7.0
958
7.5
748
8.0
546
8.5
347
9.0
107
9.5
pChEMBL
Approved Drugs

Approved Drugs

INAVOLISIB
CHEMBL4650215
Approved 2024
LENIOLISIB
CHEMBL3643413
Approved 2023
ALPELISIB
CHEMBL2396661
Approved 2019
DUVELISIB
CHEMBL3039502
Approved 2018
COPANLISIB
CHEMBL3218576
Approved 2017
COPANLISIB HYDROCHLORIDE
CHEMBL3545068
Approved 2017
IDELALISIB
CHEMBL2216870
Approved 2014
CRIZOTINIB
CHEMBL601719
Approved 2011
Assay Landscape

Assay Landscape

1,726
Total Assays
8,127
Tested Compounds
4
Assay Types
Binding — 1,710 assays, 8,127 compounds
BAO Format Assays Compounds Avg pChEMBL
single protein format 1,176 6,628 6.9
assay format 297 458 6.5
cell-based format 236 1,041 7.1
subcellular format 1 0
ADME — 10 assays, 47 compounds
BAO Format Assays Compounds Avg pChEMBL
single protein format 7 36 6.4
cell-based format 3 11 5.4
Toxicity — 4 assays, 6 compounds
BAO Format Assays Compounds Avg pChEMBL
assay format 4 6 5.7
Functional — 2 assays, 1 compounds
BAO Format Assays Compounds Avg pChEMBL
assay format 2 1 6.8

Confidence Score Distribution

Source · ChEMBL 36 via Core Engine