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Assay Detail

CHEMBL3366680

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

Binding
Inhibition of PI3Kgamma (unknown origin) assessed as decrease in fluorescence intensity using phosphorylated substrate
98
Total Activities
98
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

Discovery of nanomolar phosphoinositide 3-kinase gamma (PI3Kγ) inhibitors using ligand-based modeling and virtual screening followed by in vitro analysis.
Taha MO, Al-Sha'er MA, Khanfar MA, Al-Nadaf AH.
Eur J Med Chem (2014) 84 : 454 -465
PubMed 25050878 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 98 6.39 8.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL393121 1 8.09
CHEMBL246440 1 8.00
CHEMBL241710 1 7.99
CHEMBL392349 1 7.96
CHEMBL394234 1 7.95
CHEMBL246859 1 7.95
CHEMBL394235 1 7.93
CHEMBL246441 1 7.75
CHEMBL392914 1 7.74
CHEMBL246647 1 7.74
CHEMBL211819 1 7.70
CHEMBL241718 1 7.70
CHEMBL211173 1 7.70
CHEMBL429657 1 7.69
CHEMBL246857 1 7.68
CHEMBL398988 1 7.56
CHEMBL3325884 1 7.54
CHEMBL208652 1 7.52
CHEMBL393276 1 7.52
CHEMBL379156 1 7.48
CHEMBL239374 1 7.43
CHEMBL377175 1 7.43
CHEMBL377104 1 7.41
CHEMBL378999 1 7.40
CHEMBL212119 1 7.37
CHEMBL211768 1 7.25
CHEMBL210991 1 7.10
CHEMBL391998 1 7.01
CHEMBL240623 1 6.99
CHEMBL378528 1 6.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL393121 IC50 = 8.1 nM 8.09
CHEMBL246440 IC50 = 9.9 nM 8.00
CHEMBL241710 IC50 = 10.2 nM 7.99
CHEMBL392349 IC50 = 11.0 nM 7.96
CHEMBL394234 IC50 = 11.2 nM 7.95
CHEMBL246859 IC50 = 11.22 nM 7.95
CHEMBL394235 IC50 = 11.8 nM 7.93
CHEMBL246441 IC50 = 18.0 nM 7.75
CHEMBL392914 IC50 = 18.4 nM 7.74
CHEMBL246647 IC50 = 18.1 nM 7.74
CHEMBL211819 IC50 = 20.0 nM 7.70
CHEMBL241718 IC50 = 20.1 nM 7.70
CHEMBL211173 IC50 = 20.0 nM 7.70
CHEMBL429657 IC50 = 20.43 nM 7.69
CHEMBL246857 IC50 = 20.9 nM 7.68
CHEMBL398988 IC50 = 27.7 nM 7.56
CHEMBL3325884 IC50 = 29.0 nM 7.54
CHEMBL208652 IC50 = 30.0 nM 7.52
CHEMBL393276 IC50 = 30.0 nM 7.52
CHEMBL379156 IC50 = 33.0 nM 7.48
CHEMBL239374 IC50 = 37.3 nM 7.43
CHEMBL377175 IC50 = 37.0 nM 7.43
CHEMBL377104 IC50 = 39.0 nM 7.41
CHEMBL378999 IC50 = 40.0 nM 7.40
CHEMBL212119 IC50 = 43.0 nM 7.37
CHEMBL211768 IC50 = 56.0 nM 7.25
CHEMBL210991 IC50 = 80.0 nM 7.10
CHEMBL391998 IC50 = 97.0 nM 7.01
CHEMBL240623 IC50 = 103.4 nM 6.99
CHEMBL378528 IC50 = 110.0 nM 6.96
CHEMBL240620 IC50 = 116.0 nM 6.94
CHEMBL241708 IC50 = 124.0 nM 6.91
CHEMBL246645 IC50 = 140.0 nM 6.85
CHEMBL241713 IC50 = 152.4 nM 6.82
CHEMBL240621 IC50 = 184.5 nM 6.73
CHEMBL437688 IC50 = 200.0 nM 6.70
CHEMBL211068 IC50 = 260.0 nM 6.58
CHEMBL208662 IC50 = 290.0 nM 6.54
CHEMBL438133 IC50 = 328.0 nM 6.48
CHEMBL211759 IC50 = 380.0 nM 6.42
CHEMBL208696 IC50 = 530.0 nM 6.28
CHEMBL209194 IC50 = 840.0 nM 6.08
CHEMBL377337 IC50 = 920.0 nM 6.04
CHEMBL376984 IC50 = 950.0 nM 6.02
CHEMBL211112 IC50 = 1000.0 nM 6.00
CHEMBL208866 IC50 = 1200.0 nM 5.92
CHEMBL3326777 IC50 = 1820.0 nM 5.74
CHEMBL1213083 IC50 = 2030.0 nM 5.69
CHEMBL3326383 IC50 = 2540.0 nM 5.59
CHEMBL209409 IC50 = 2600.0 nM 5.58