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Assay Detail

CHEMBL2020155

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

Functional
Antiproliferative activity against human A2780 cells after 3 days by CellTiter-Glo assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type A2780
Confidence 1 — Organism
Curated By Autocuration

Target

A2780 (CHEMBL614004)
Type CELL-LINE
Organism Homo sapiens

Publication

Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer.
Burger MT, Pecchi S, Wagman A, Ni ZJ, Knapp M, Hendrickson T, Atallah G, Pfister K, Zhang Y, Bartulis S, Frazier K, Ng S, Smith A, Verhagen J, Haznedar J, Huh K, Iwanowicz E, Xin X, Menezes D, Merritt H, Lee I, Wiesmann M, Kaufman S, Crawford K, Chin M, Bussiere D, Shoemaker K, Zaror I, Maira SM, Voliva CF.
ACS Med Chem Lett (2011) 2 : 774 -779
PubMed 24900266 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 6.34 7.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2017967 1 7.08
CHEMBL1672323 1 6.84
CHEMBL2017968 1 6.77
CHEMBL2017966 1 6.72
CHEMBL2016592 1 6.72
CHEMBL2017965 1 6.55
CHEMBL2017977 1 6.35
CHEMBL2017973 1 6.29
CHEMBL2017974 BUPARLISIB 3.0 1 6.28
CHEMBL1672316 1 6.27
CHEMBL2017970 1 6.24
CHEMBL2017976 1 6.17
CHEMBL2017971 1 6.03
CHEMBL2017975 1 5.84
CHEMBL2017972 1 5.75
CHEMBL2017969 1 5.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2017967 EC50 = 83.0 nM 7.08
CHEMBL1672323 EC50 = 146.0 nM 6.84
CHEMBL2017968 EC50 = 170.0 nM 6.77
CHEMBL2017966 EC50 = 190.0 nM 6.72
CHEMBL2016592 EC50 = 190.0 nM 6.72
CHEMBL2017965 EC50 = 280.0 nM 6.55
CHEMBL2017977 EC50 = 450.0 nM 6.35
CHEMBL2017973 EC50 = 510.0 nM 6.29
CHEMBL2017974 BUPARLISIB EC50 = 520.0 nM 6.28
CHEMBL1672316 EC50 = 540.0 nM 6.27
CHEMBL2017970 EC50 = 580.0 nM 6.24
CHEMBL2017976 EC50 = 680.0 nM 6.17
CHEMBL2017971 EC50 = 930.0 nM 6.03
CHEMBL2017975 EC50 = 1460.0 nM 5.84
CHEMBL2017972 EC50 = 1770.0 nM 5.75
CHEMBL2017969 EC50 = 3200.0 nM 5.50