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Assay Detail

CHEMBL3705490

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Binding
Enzyme Assay: Test of Lipid Kinase Activity: The kinase reaction is performed in a final volume of 50 μl per well of a half area COSTAR, 96 well plate. The final concentrations of ATP and phosphatidyl inositol in the assay are 5 μM and 6 μg/mL, respectively. The reaction is started by the addition of PI3 kinase, e.g. PI3 kinase δ. Refer to the patent for more info.
ChEMBL ↗
94
Total Activities
94
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

Target

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (CHEMBL4005) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tetrahydro-pyrido-pyrimidine derivatives
(2014)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 94 6.09 7.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3643414 — — 1 7.37
CHEMBL3643419 — — 1 7.27
CHEMBL3643415 — — 1 7.25
CHEMBL3643417 — — 1 7.24
CHEMBL3643430 — — 1 7.24
CHEMBL3643428 — — 1 7.18
CHEMBL3643418 — — 1 7.03
CHEMBL3643422 — — 1 6.97
CHEMBL3643420 — — 1 6.95
CHEMBL3643421 — — 1 6.93
CHEMBL3643416 — — 1 6.92
CHEMBL3643371 — — 1 6.89
CHEMBL3643387 — — 1 6.58
CHEMBL3643413 LENIOLISIB 4.0 1 6.58
CHEMBL3643369 — — 1 6.50
CHEMBL3643372 — — 1 6.43
CHEMBL3643373 — — 1 6.43
CHEMBL3643400 — — 1 6.42
CHEMBL3643424 — — 1 6.42
CHEMBL3643396 — — 1 6.41
CHEMBL3643426 — — 1 6.37
CHEMBL3643429 — — 1 6.37
CHEMBL3643386 — — 1 6.36
CHEMBL3643433 — — 1 6.34
CHEMBL3643408 — — 1 6.31
CHEMBL3643399 — — 1 6.30
CHEMBL3643395 — — 1 6.29
CHEMBL3643388 — — 1 6.29
CHEMBL3643431 — — 1 6.25
CHEMBL3643370 — — 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3643414 — IC50 = 43.0 nM 7.37
CHEMBL3643419 — IC50 = 54.0 nM 7.27
CHEMBL3643415 — IC50 = 56.0 nM 7.25
CHEMBL3643417 — IC50 = 57.0 nM 7.24
CHEMBL3643430 — IC50 = 58.0 nM 7.24
CHEMBL3643428 — IC50 = 66.0 nM 7.18
CHEMBL3643418 — IC50 = 93.0 nM 7.03
CHEMBL3643422 — IC50 = 106.0 nM 6.97
CHEMBL3643420 — IC50 = 113.0 nM 6.95
CHEMBL3643421 — IC50 = 118.0 nM 6.93
CHEMBL3643416 — IC50 = 121.0 nM 6.92
CHEMBL3643371 — IC50 = 129.0 nM 6.89
CHEMBL3643387 — IC50 = 260.0 nM 6.58
CHEMBL3643413 LENIOLISIB IC50 = 262.0 nM 6.58
CHEMBL3643369 — IC50 = 320.0 nM 6.50
CHEMBL3643372 — IC50 = 374.0 nM 6.43
CHEMBL3643373 — IC50 = 368.0 nM 6.43
CHEMBL3643400 — IC50 = 384.0 nM 6.42
CHEMBL3643424 — IC50 = 384.0 nM 6.42
CHEMBL3643396 — IC50 = 388.0 nM 6.41
CHEMBL3643426 — IC50 = 430.0 nM 6.37
CHEMBL3643429 — IC50 = 432.0 nM 6.37
CHEMBL3643386 — IC50 = 434.0 nM 6.36
CHEMBL3643433 — IC50 = 452.0 nM 6.34
CHEMBL3643408 — IC50 = 489.0 nM 6.31
CHEMBL3643399 — IC50 = 504.0 nM 6.30
CHEMBL3643388 — IC50 = 515.0 nM 6.29
CHEMBL3643395 — IC50 = 518.0 nM 6.29
CHEMBL3643431 — IC50 = 569.0 nM 6.25
CHEMBL3643370 — IC50 = 580.0 nM 6.24
CHEMBL3643403 — IC50 = 590.0 nM 6.23
CHEMBL3643407 — IC50 = 589.0 nM 6.23
CHEMBL3643427 — IC50 = 651.0 nM 6.19
CHEMBL3643394 — IC50 = 656.0 nM 6.18
CHEMBL3643401 — IC50 = 661.0 nM 6.18
CHEMBL3643358 — IC50 = 668.0 nM 6.17
CHEMBL3643390 — IC50 = 728.0 nM 6.14
CHEMBL3643353 — IC50 = 749.0 nM 6.13
CHEMBL3643411 — IC50 = 738.0 nM 6.13
CHEMBL3643441 — IC50 = 757.0 nM 6.12
CHEMBL3643425 — IC50 = 781.0 nM 6.11
CHEMBL3643409 — IC50 = 791.0 nM 6.10
CHEMBL3639422 — IC50 = 820.0 nM 6.09
CHEMBL3643393 — IC50 = 803.0 nM 6.09
CHEMBL3643402 — IC50 = 860.0 nM 6.07
CHEMBL3643392 — IC50 = 860.0 nM 6.07
CHEMBL3643439 — IC50 = 872.0 nM 6.06
CHEMBL3643366 — IC50 = 871.0 nM 6.06
CHEMBL3643389 — IC50 = 863.0 nM 6.06
CHEMBL3643397 — IC50 = 912.0 nM 6.04