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Assay Detail

CHEMBL3136756

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Binding
Inhibition of human PI3Kgamma
ChEMBL ↗
43
Total Activities
22
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 gamma isoform (CHEMBL3267) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of a novel series of N,4-diphenylpyrimidin-2-amine derivatives as potent and selective PI3K inhibitors
Yang H, Fang F, Zhao C, Li D, Li J, Sun J, Du Q, Zhu H
Medchemcomm (2014) 5 : 219 -225
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 43 6.61 7.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3134612 — — 2 7.19
CHEMBL244559 — — 1 6.90
CHEMBL3134607 — — 2 6.84
CHEMBL3134620 — — 2 6.81
CHEMBL3134606 — — 2 6.78
CHEMBL3134605 — — 2 6.71
CHEMBL3134619 — — 2 6.66
CHEMBL3134618 — — 2 6.64
CHEMBL3134608 — — 2 6.63
CHEMBL3134611 — — 2 6.61
CHEMBL3134621 — — 2 6.60
CHEMBL3134617 — — 2 6.58
CHEMBL3134604 — — 2 6.57
CHEMBL3134601 — — 2 6.56
CHEMBL3134602 — — 2 6.56
CHEMBL3134616 — — 2 6.52
CHEMBL3134615 — — 2 6.50
CHEMBL3134610 — — 2 6.48
CHEMBL3134613 — — 2 6.47
CHEMBL3134614 — — 2 6.45
CHEMBL3134609 — — 2 6.43
CHEMBL3134603 — — 2 6.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3134612 — IC50 = 65.0 nM 7.19
CHEMBL244559 — IC50 = 127.0 nM 6.90
CHEMBL3134607 — IC50 = 142.99 nM 6.84
CHEMBL3134607 — IC50 = 143.0 nM 6.84
CHEMBL3134620 — IC50 = 154.0 nM 6.81
CHEMBL3134620 — IC50 = 153.99 nM 6.81
CHEMBL3134606 — IC50 = 167.0 nM 6.78
CHEMBL3134606 — IC50 = 166.99 nM 6.78
CHEMBL3134605 — IC50 = 195.0 nM 6.71
CHEMBL3134605 — IC50 = 194.98 nM 6.71
CHEMBL3134619 — IC50 = 217.02 nM 6.66
CHEMBL3134619 — IC50 = 217.0 nM 6.66
CHEMBL3134618 — IC50 = 230.99 nM 6.64
CHEMBL3134618 — IC50 = 231.0 nM 6.64
CHEMBL3134608 — IC50 = 235.0 nM 6.63
CHEMBL3134608 — IC50 = 235.02 nM 6.63
CHEMBL3134611 — IC50 = 247.0 nM 6.61
CHEMBL3134611 — IC50 = 247.0 nM 6.61
CHEMBL3134621 — IC50 = 250.0 nM 6.60
CHEMBL3134621 — IC50 = 249.98 nM 6.60
CHEMBL3134617 — IC50 = 265.0 nM 6.58
CHEMBL3134617 — IC50 = 264.97 nM 6.58
CHEMBL3134604 — IC50 = 268.0 nM 6.57
CHEMBL3134604 — IC50 = 267.98 nM 6.57
CHEMBL3134601 — IC50 = 274.03 nM 6.56
CHEMBL3134601 — IC50 = 274.0 nM 6.56
CHEMBL3134602 — IC50 = 278.0 nM 6.56
CHEMBL3134602 — IC50 = 277.97 nM 6.56
CHEMBL3134616 — IC50 = 302.0 nM 6.52
CHEMBL3134616 — IC50 = 302.0 nM 6.52
CHEMBL3134615 — IC50 = 313.0 nM 6.50
CHEMBL3134615 — IC50 = 312.97 nM 6.50
CHEMBL3134610 — IC50 = 334.0 nM 6.48
CHEMBL3134610 — IC50 = 333.96 nM 6.48
CHEMBL3134613 — IC50 = 342.0 nM 6.47
CHEMBL3134613 — IC50 = 341.98 nM 6.47
CHEMBL3134614 — IC50 = 357.0 nM 6.45
CHEMBL3134614 — IC50 = 357.03 nM 6.45
CHEMBL3134609 — IC50 = 371.02 nM 6.43
CHEMBL3134609 — IC50 = 371.0 nM 6.43
CHEMBL3134603 — IC50 = 386.01 nM 6.41
CHEMBL3134603 — IC50 = 386.0 nM 6.41
CHEMBL3134612 — IC50 <= 65.0 nM -