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Assay Detail

CHEMBL5587989

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

Binding
Inhibition of PI3Kdelta (unknown origin) using PI3:PS as substrate incubated for 1 hr in presence of ATP by ADP-glo kinase assay
26
Total Activities
26
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 Pyrazolo[1,5-<i>a</i>]pyridine Derivatives as Potent and Selective PI3Kγ/δ Inhibitors.
Wang C, Zou F, Qi Z, Liu Q, Shen L, Yuan X, Deng M, Wang A, Wang B, Wang L, Liang X, Liu Q, Liu J.
J Med Chem (2024) 67 : 15199 -15219
PubMed 39163191 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 7.75 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5598454 1 8.80
CHEMBL5590633 1 8.52
CHEMBL5598309 1 8.48
CHEMBL5597159 1 8.40
CHEMBL5596579 1 8.29
CHEMBL5596530 1 8.28
CHEMBL5597293 1 8.22
CHEMBL5597786 1 8.10
CHEMBL5597218 1 8.04
CHEMBL5598183 1 8.01
CHEMBL5598560 1 7.97
CHEMBL5596735 1 7.80
CHEMBL5597286 1 7.78
CHEMBL5596114 1 7.75
CHEMBL5590113 1 7.69
CHEMBL5596364 1 7.67
CHEMBL5597371 1 7.57
CHEMBL5597160 1 7.49
CHEMBL5590382 1 7.45
CHEMBL5596470 1 7.40
CHEMBL5596476 1 7.20
CHEMBL5596611 1 7.18
CHEMBL5597610 1 7.16
CHEMBL5596396 1 6.96
CHEMBL5597903 1 6.94
CHEMBL5596701 1 6.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5598454 IC50 = 1.6 nM 8.80
CHEMBL5590633 IC50 = 3.0 nM 8.52
CHEMBL5598309 IC50 = 3.3 nM 8.48
CHEMBL5597159 IC50 = 4.0 nM 8.40
CHEMBL5596579 IC50 = 5.1 nM 8.29
CHEMBL5596530 IC50 = 5.2 nM 8.28
CHEMBL5597293 IC50 = 6.0 nM 8.22
CHEMBL5597786 IC50 = 7.9 nM 8.10
CHEMBL5597218 IC50 = 9.1 nM 8.04
CHEMBL5598183 IC50 = 9.8 nM 8.01
CHEMBL5598560 IC50 = 10.8 nM 7.97
CHEMBL5596735 IC50 = 15.7 nM 7.80
CHEMBL5597286 IC50 = 16.6 nM 7.78
CHEMBL5596114 IC50 = 17.7 nM 7.75
CHEMBL5590113 IC50 = 20.6 nM 7.69
CHEMBL5596364 IC50 = 21.4 nM 7.67
CHEMBL5597371 IC50 = 26.8 nM 7.57
CHEMBL5597160 IC50 = 32.5 nM 7.49
CHEMBL5590382 IC50 = 35.8 nM 7.45
CHEMBL5596470 IC50 = 39.6 nM 7.40
CHEMBL5596476 IC50 = 62.6 nM 7.20
CHEMBL5596611 IC50 = 66.2 nM 7.18
CHEMBL5597610 IC50 = 69.7 nM 7.16
CHEMBL5596396 IC50 = 108.9 nM 6.96
CHEMBL5597903 IC50 = 114.2 nM 6.94
CHEMBL5596701 IC50 = 521.9 nM 6.28