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Assay Detail

CHEMBL2415771

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

Binding
Inhibition of PI3Kdelta (unknown origin) assessed as formation of PIP3 by competitive fluorescence polarization assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Identification of GNE-293, a potent and selective PI3Kδ inhibitor: navigating in vitro genotoxicity while improving potency and selectivity.
Safina BS, Sweeney ZK, Li J, Chan BK, Bisconte A, Carrera D, Castanedo G, Flagella M, Heald R, Lewis C, Murray JM, Nonomiya J, Pang J, Price S, Reif K, Salphati L, Seward EM, Wei B, Sutherlin DP.
Bioorg Med Chem Lett (2013) 23 : 4953 -4959
PubMed 23867164 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 8.91 9.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2414299 1 9.64
CHEMBL2414301 1 9.44
CHEMBL2216902 1 9.33
CHEMBL2216903 1 9.24
CHEMBL2414297 1 9.23
CHEMBL2414294 1 9.10
CHEMBL2414300 1 9.06
CHEMBL2414298 1 9.05
CHEMBL2414238 1 8.96
CHEMBL2171939 1 8.74
CHEMBL2171952 1 8.70
CHEMBL2171944 1 8.70
CHEMBL2414239 1 8.64
CHEMBL2414296 1 8.51
CHEMBL2165501 1 8.26
CHEMBL2414295 1 7.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2414299 Ki = 0.23 nM 9.64
CHEMBL2414301 Ki = 0.36 nM 9.44
CHEMBL2216902 Ki = 0.47 nM 9.33
CHEMBL2216903 Ki = 0.58 nM 9.24
CHEMBL2414297 Ki = 0.59 nM 9.23
CHEMBL2414294 Ki = 0.8 nM 9.10
CHEMBL2414300 Ki = 0.88 nM 9.06
CHEMBL2414298 Ki = 0.9 nM 9.05
CHEMBL2414238 Ki = 1.1 nM 8.96
CHEMBL2171939 Ki = 1.8 nM 8.74
CHEMBL2171952 Ki = 2.0 nM 8.70
CHEMBL2171944 Ki = 2.0 nM 8.70
CHEMBL2414239 Ki = 2.3 nM 8.64
CHEMBL2414296 Ki = 3.1 nM 8.51
CHEMBL2165501 Ki = 5.5 nM 8.26
CHEMBL2414295 Ki = 12.7 nM 7.90