Assay Detail

CHEMBL4724072

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Functional

Anticancer activity against human OCILY10 assessed as inhibition of ATP level measured after 96 hrs by CellTiter-Glo reagent assay

ChEMBL ↗

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Target

OCI-Ly10 (CHEMBL4483285) ↗

Open DB target context

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OCI-Ly10 (CHEMBL4483285) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target OCI-Ly10

CHEMBL4483285

Anchored from Assay target.

Protein identity OCI-Ly10

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Functional
Organism	Homo sapiens
Cell Type	OCI-Ly10
Confidence	1 — Organism
Curated By	Autocuration

Target

OCI-Ly10 (CHEMBL4483285) ↗

Type	CELL-LINE
Organism	Homo sapiens

Publication

Discovery of a Potent and Selective PI3Kδ Inhibitor (S)-2,4-Diamino-6-((1-(7-fluoro-1-(4-fluorophenyl)-4-oxo-3-phenyl-4H-quinolizin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile with Improved Pharmacokinetic Profile and Superior Efficacy in Hematological Cancer Models.

Shukla MR,Patra S,Verma M,Sadasivam G,Jana N,Mahangare SJ,Vidhate P,Lagad D,Tarage A,Cheemala M,Kulkarni C,Bhagwat S,Chaudhari VD,Sayyed M,Pachpute V,Phadtare R,Gole G,Phukan S,Sunkara B,Samant C,Shingare M,Naik A,Trivedi S,Marisetti AK,Reddy M,Gholve M,Mahajan N,Sabde S,Patil V,Modi D,Mehta M,Nigade P,Tamane K,Tota S,Goyal H,Volam H,Pawar S,Ahirrao P,Dinchhana L,Mallurwar S,Akarte A,Bokare A,Kanhere R,Reddy N,Koul S,Dandekar M,Singh M,Bernstein PR,Narasimham L,Bhonde M,Gundu J,Goel R,Kulkarni S,Sharma S,Kamboj RK,Palle VP
J Med Chem (2020) 63 : 14700 -14723
PubMed 33297683 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	4	8.13	8.74

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4794328	—	—	1	8.74
CHEMBL4755417	—	—	1	8.15
CHEMBL2216870	IDELALISIB	4.0	1	7.50
CHEMBL4756563	—	—	1	-

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4794328	—	IC50	=	1.8	nM	8.74
CHEMBL4755417	—	IC50	=	7.02	nM	8.15
CHEMBL2216870	IDELALISIB	IC50	=	31.9	nM	7.50
CHEMBL4756563	—	IC50	<	1.0	nM	-