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Assay Detail

CHEMBL4024911

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Binding
Inhibition of PI3Kdelta in ACD-treated human whole blood assessed as reduction in CD69 expression measured after 1 hr
25
Total Activities
25
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 highly potent and selective PI3Kδ inhibitors.
Marcoux D, Qin LY, Ruan Z, Shi Q, Ruan Q, Weigelt C, Qiu H, Schieven G, Hynes J, Bhide R, Poss M, Tino J.
Bioorg Med Chem Lett (2017) 27 : 2849 -2853
PubMed 28209465 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 7.14 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4091875 1 8.15
CHEMBL4096456 1 7.89
CHEMBL4061320 1 7.58
CHEMBL4071039 1 7.52
CHEMBL4105636 1 7.52
CHEMBL4077248 1 7.50
CHEMBL4089489 1 7.48
CHEMBL4099608 1 7.46
CHEMBL4090297 1 7.38
CHEMBL4072098 1 7.36
CHEMBL4080090 1 7.35
CHEMBL4065999 1 7.35
CHEMBL4060977 1 7.30
CHEMBL4084394 1 7.11
CHEMBL4077544 1 7.11
CHEMBL4081613 1 7.04
CHEMBL4076745 1 6.92
CHEMBL4101245 1 6.89
CHEMBL4067250 1 6.77
CHEMBL4069993 1 6.62
CHEMBL4097187 1 6.62
CHEMBL4069213 1 6.58
CHEMBL4092654 1 6.54
CHEMBL4093593 1 6.41
CHEMBL4086343 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4091875 IC50 = 7.0 nM 8.15
CHEMBL4096456 IC50 = 13.0 nM 7.89
CHEMBL4061320 IC50 = 26.0 nM 7.58
CHEMBL4071039 IC50 = 30.0 nM 7.52
CHEMBL4105636 IC50 = 30.0 nM 7.52
CHEMBL4077248 IC50 = 32.0 nM 7.50
CHEMBL4089489 IC50 = 33.0 nM 7.48
CHEMBL4099608 IC50 = 35.0 nM 7.46
CHEMBL4090297 IC50 = 42.0 nM 7.38
CHEMBL4072098 IC50 = 44.0 nM 7.36
CHEMBL4080090 IC50 = 45.0 nM 7.35
CHEMBL4065999 IC50 = 45.0 nM 7.35
CHEMBL4060977 IC50 = 50.0 nM 7.30
CHEMBL4084394 IC50 = 77.0 nM 7.11
CHEMBL4077544 IC50 = 78.0 nM 7.11
CHEMBL4081613 IC50 = 91.0 nM 7.04
CHEMBL4076745 IC50 = 120.0 nM 6.92
CHEMBL4101245 IC50 = 130.0 nM 6.89
CHEMBL4067250 IC50 = 170.0 nM 6.77
CHEMBL4069993 IC50 = 240.0 nM 6.62
CHEMBL4097187 IC50 = 240.0 nM 6.62
CHEMBL4069213 IC50 = 260.0 nM 6.58
CHEMBL4092654 IC50 = 290.0 nM 6.54
CHEMBL4093593 IC50 = 390.0 nM 6.41
CHEMBL4086343 IC50 = 1000.0 nM 6.00