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Assay Detail

CHEMBL5731586

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Binding
p110alpha (Alpha) PI3K Binding Assay: PI3K Binding assays are intended for determining the biochemical potency of small molecule PI3K inhibitors. The PI3K lipid kinase reaction is performed in the presence of PIP2:3PS lipid substrate (Promega #V1792) and ATP. Following the termination if the kinase reaction, turnover of ATP to ADP by the phosphorylation of the lipid substrate is detected using the Promega ADP-Glo (Promega #V1792) assay. ReactionFinal Kinase ATP PIP2:3PS TimeKinase Source Concentration (uM) (uM) (min.)PI3K alpha Millipore 0.2 nM 40 50 120#14-602-K PI3K beta Promega 0.6 nM 40 50 120#V1751 PI3K delta Millipore 0.25 nM  40 50 120#14-604-K PI3K gamma Millipore 0.4 nM 25 50 120#14-558-KAfter 120 minutes of reaction time, the kinase reaction is terminated. Any ATP remaining after the reaction is depleted, leaving only ADP. Then the Kinase Detection Reagent is added to convert ADP to ATP, which is used in a coupled luciferin/luciferase reaction. The luminescent output is measured and is correlated with kinase activity.
ChEMBL ↗
66
Total Activities
20
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

Benzoxazepin oxazolidinone compounds and methods of use
(2018)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 9.51 10.80
kon 22 - -
k_off 22 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3770993 — — 3 10.80
CHEMBL6019298 — — 3 10.64
CHEMBL4650215 INAVOLISIB 4.0 3 10.47
CHEMBL5916599 — — 3 10.40
CHEMBL5789652 — — 3 10.32
CHEMBL5186155 — — 3 10.29
CHEMBL5196718 — — 3 10.22
CHEMBL2387080 TASELISIB 3.0 6 10.05
CHEMBL5916419 — — 3 9.97
CHEMBL5171276 — — 3 9.73
CHEMBL3771364 — — 3 9.46
CHEMBL5784355 — — 3 9.36
CHEMBL5967979 — — 3 9.33
CHEMBL5967345 — — 6 9.25
CHEMBL5784302 — — 3 9.02
CHEMBL5748747 — — 3 9.02
CHEMBL521851 PICTILISIB 2.0 3 8.59
CHEMBL5916259 — — 3 8.56
CHEMBL5875257 — — 3 8.45
CHEMBL5847452 — — 3 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3770993 — Ki = 0.016 nM 10.80
CHEMBL6019298 — Ki = 0.023 nM 10.64
CHEMBL4650215 INAVOLISIB Ki = 0.034 nM 10.47
CHEMBL5916599 — Ki = 0.04 nM 10.40
CHEMBL5789652 — Ki = 0.048 nM 10.32
CHEMBL5186155 — Ki = 0.051 nM 10.29
CHEMBL5196718 — Ki = 0.06 nM 10.22
CHEMBL2387080 TASELISIB Ki = 0.09 nM 10.05
CHEMBL5916419 — Ki = 0.107 nM 9.97
CHEMBL5171276 — Ki = 0.186 nM 9.73
CHEMBL3771364 — Ki = 0.35 nM 9.46
CHEMBL5784355 — Ki = 0.437 nM 9.36
CHEMBL5967979 — Ki = 0.464 nM 9.33
CHEMBL5967345 — Ki = 0.56 nM 9.25
CHEMBL5748747 — Ki = 0.949 nM 9.02
CHEMBL5784302 — Ki = 0.967 nM 9.02
CHEMBL521851 PICTILISIB Ki = 2.56 nM 8.59
CHEMBL5916259 — Ki = 2.72 nM 8.56
CHEMBL5875257 — Ki = 3.56 nM 8.45
CHEMBL5967345 — Ki = 5.66 nM 8.25
CHEMBL2387080 TASELISIB Ki = 23.7 nM 7.62
CHEMBL5967345 — kon = - — -
CHEMBL5967345 — k_off = - s-1 -
CHEMBL5967345 — kon = - — -
CHEMBL5186155 — k_off = - s-1 -
CHEMBL2387080 TASELISIB kon = - — -
CHEMBL2387080 TASELISIB k_off = - s-1 -
CHEMBL521851 PICTILISIB kon = - — -
CHEMBL521851 PICTILISIB k_off = - s-1 -
CHEMBL4650215 INAVOLISIB kon = - — -
CHEMBL4650215 INAVOLISIB k_off = - s-1 -
CHEMBL5748747 — kon = - — -
CHEMBL5748747 — k_off = - s-1 -
CHEMBL5196718 — kon = - — -
CHEMBL5196718 — k_off = - s-1 -
CHEMBL5916419 — kon = - — -
CHEMBL5784355 — k_off = - s-1 -
CHEMBL5784355 — kon = - — -
CHEMBL5916419 — k_off = - s-1 -
CHEMBL5916259 — k_off = - s-1 -
CHEMBL5916259 — kon = - — -
CHEMBL6019298 — k_off = - s-1 -
CHEMBL5967345 — k_off = - s-1 -
CHEMBL5171276 — kon = - — -
CHEMBL5171276 — k_off = - s-1 -
CHEMBL5784302 — k_off = - s-1 -
CHEMBL5875257 — k_off = - s-1 -
CHEMBL5784302 — kon = - — -
CHEMBL6019298 — kon = - — -
CHEMBL5875257 — kon = - — -