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Assay Detail

CHEMBL3587457

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Inhibition of cell proliferation of human NZOV9 cells containing wild-type p53 protein and p110alpha Y1021C mutant incubated for 5 days by [3H]thymidine incorporation assay
ChEMBL ↗
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NZOV9
Confidence 1 — Organism
Curated By Autocuration

Target

NON-PROTEIN TARGET (CHEMBL3879801) ↗
Type NON-MOLECULAR

Publication

Exploring the isoform selectivity of TGX-221 related pyrido[1,2-a]pyrimidinone-based Class IA PI 3-kinase inhibitors: synthesis, biological evaluation and molecular modelling.
Marshall AJ, Lill CL, Chao M, Kolekar SV, Lee WJ, Marshall ES, Baguley BC, Shepherd PR, Denny WA, Flanagan JU, Rewcastle GW.
Bioorg Med Chem (2015) 23 : 3796 -3808
PubMed 25890698 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 5.51 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3585601 — — 1 6.30
CHEMBL3585620 — — 1 6.30
CHEMBL3585607 — — 1 6.22
CHEMBL3585598 — — 1 6.22
CHEMBL3585619 — — 1 6.10
CHEMBL3585618 — — 1 6.10
CHEMBL3585617 — — 1 6.10
CHEMBL3585608 — — 1 6.10
CHEMBL1972466 — — 1 5.92
CHEMBL3585602 — — 1 5.89
CHEMBL3585600 — — 1 5.89
CHEMBL3585599 — — 1 5.80
CHEMBL3585597 — — 1 5.66
CHEMBL3585622 — — 1 5.60
CHEMBL3585616 — — 1 5.60
CHEMBL3585611 — — 1 5.55
CHEMBL3585621 — — 1 5.54
CHEMBL3585595 — — 1 5.52
CHEMBL3585596 — — 1 5.30
CHEMBL3218574 — — 1 5.30
CHEMBL3585586 — — 1 5.24
CHEMBL3585590 — — 1 5.20
CHEMBL3585609 — — 1 5.16
CHEMBL3585604 — — 1 5.16
CHEMBL3585605 — — 1 5.10
CHEMBL3585592 — — 1 5.09
CHEMBL3585588 — — 1 5.02
CHEMBL3585583 — — 1 5.00
CHEMBL3585591 — — 1 4.96
CHEMBL3585610 — — 1 4.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3585601 — IC50 = 500.0 nM 6.30
CHEMBL3585620 — IC50 = 500.0 nM 6.30
CHEMBL3585598 — IC50 = 600.0 nM 6.22
CHEMBL3585607 — IC50 = 600.0 nM 6.22
CHEMBL3585619 — IC50 = 800.0 nM 6.10
CHEMBL3585618 — IC50 = 800.0 nM 6.10
CHEMBL3585617 — IC50 = 800.0 nM 6.10
CHEMBL3585608 — IC50 = 800.0 nM 6.10
CHEMBL1972466 — IC50 = 1200.0 nM 5.92
CHEMBL3585602 — IC50 = 1300.0 nM 5.89
CHEMBL3585600 — IC50 = 1300.0 nM 5.89
CHEMBL3585599 — IC50 = 1600.0 nM 5.80
CHEMBL3585597 — IC50 = 2200.0 nM 5.66
CHEMBL3585622 — IC50 = 2500.0 nM 5.60
CHEMBL3585616 — IC50 = 2500.0 nM 5.60
CHEMBL3585611 — IC50 = 2800.0 nM 5.55
CHEMBL3585621 — IC50 = 2900.0 nM 5.54
CHEMBL3585595 — IC50 = 3000.0 nM 5.52
CHEMBL3585596 — IC50 = 5000.0 nM 5.30
CHEMBL3218574 — IC50 = 5000.0 nM 5.30
CHEMBL3585586 — IC50 = 5800.0 nM 5.24
CHEMBL3585590 — IC50 = 6300.0 nM 5.20
CHEMBL3585609 — IC50 = 7000.0 nM 5.16
CHEMBL3585604 — IC50 = 7000.0 nM 5.16
CHEMBL3585605 — IC50 = 7900.0 nM 5.10
CHEMBL3585592 — IC50 = 8200.0 nM 5.09
CHEMBL3585588 — IC50 = 9600.0 nM 5.02
CHEMBL3585583 — IC50 = 10000.0 nM 5.00
CHEMBL3585591 — IC50 = 11000.0 nM 4.96
CHEMBL3585610 — IC50 = 11000.0 nM 4.96
CHEMBL3585606 — IC50 = 14000.0 nM 4.85
CHEMBL3585593 — IC50 = 14000.0 nM 4.85
CHEMBL3585587 — IC50 = 15000.0 nM 4.82
CHEMBL3585594 — IC50 = 18000.0 nM 4.75
CHEMBL3585581 — IC50 - — -
CHEMBL3585351 — IC50 > 20000.0 nM -
CHEMBL3585582 — IC50 - — -
CHEMBL3585589 — IC50 > 20000.0 nM -
CHEMBL3585584 — IC50 - — -
CHEMBL3585585 — IC50 - — -
CHEMBL3585603 — IC50 > 20000.0 nM -
CHEMBL3585615 — IC50 > 20000.0 nM -
CHEMBL3585614 — IC50 > 20000.0 nM -
CHEMBL3585613 — IC50 > 20000.0 nM -
CHEMBL3585612 — IC50 > 20000.0 nM -