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Assay Detail

CHEMBL2157136

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

Binding
Inhibition of human PI3Kdelta expressed in sf9 cells coexpressing p85alpha assessed as amount of ATP consumed by luciferase-luciferin chemiluminescence assay
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase γ inhibitors.
Leahy JW, Buhr CA, Johnson HW, Kim BG, Baik T, Cannoy J, Forsyth TP, Jeong JW, Lee MS, Ma S, Noson K, Wang L, Williams M, Nuss JM, Brooks E, Foster P, Goon L, Heald N, Holst C, Jaeger C, Lam S, Lougheed J, Nguyen L, Plonowski A, Song J, Stout T, Wu X, Yakes MF, Yu P, Zhang W, Lamb P, Raeber O.
J Med Chem (2012) 55 : 5467 -5482
PubMed 22548342 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 6.08 7.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2152257 1 7.39
CHEMBL2152139 1 7.00
CHEMBL2152256 1 6.74
CHEMBL2152148 1 6.47
CHEMBL2152130 1 6.45
CHEMBL2151050 1 6.41
CHEMBL2152141 1 6.38
CHEMBL2152253 1 6.38
CHEMBL2152144 1 6.36
CHEMBL2152127 1 6.34
CHEMBL2152136 1 6.27
CHEMBL2152146 1 6.27
CHEMBL2152142 1 6.26
CHEMBL2152140 1 6.25
CHEMBL2152132 1 6.20
CHEMBL2152252 1 6.16
CHEMBL2152250 1 6.13
CHEMBL2152126 1 6.09
CHEMBL2152145 1 5.99
CHEMBL2152150 1 5.99
CHEMBL2152131 1 5.97
CHEMBL2152129 1 5.96
CHEMBL2152124 1 5.95
CHEMBL2152149 1 5.93
CHEMBL2152134 1 5.92
CHEMBL2152147 1 5.90
CHEMBL2152255 1 5.88
CHEMBL2152143 1 5.87
CHEMBL2152133 1 5.85
CHEMBL2152135 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2152257 IC50 = 41.0 nM 7.39
CHEMBL2152139 IC50 = 100.0 nM 7.00
CHEMBL2152256 IC50 = 181.0 nM 6.74
CHEMBL2152148 IC50 = 340.0 nM 6.47
CHEMBL2152130 IC50 = 352.0 nM 6.45
CHEMBL2151050 IC50 = 387.0 nM 6.41
CHEMBL2152141 IC50 = 415.0 nM 6.38
CHEMBL2152253 IC50 = 415.0 nM 6.38
CHEMBL2152144 IC50 = 437.0 nM 6.36
CHEMBL2152127 IC50 = 456.0 nM 6.34
CHEMBL2152136 IC50 = 533.0 nM 6.27
CHEMBL2152146 IC50 = 539.0 nM 6.27
CHEMBL2152142 IC50 = 546.0 nM 6.26
CHEMBL2152140 IC50 = 568.0 nM 6.25
CHEMBL2152132 IC50 = 638.0 nM 6.20
CHEMBL2152252 IC50 = 690.0 nM 6.16
CHEMBL2152250 IC50 = 743.0 nM 6.13
CHEMBL2152126 IC50 = 816.0 nM 6.09
CHEMBL2152145 IC50 = 1020.0 nM 5.99
CHEMBL2152150 IC50 = 1032.0 nM 5.99
CHEMBL2152131 IC50 = 1073.0 nM 5.97
CHEMBL2152129 IC50 = 1095.0 nM 5.96
CHEMBL2152124 IC50 = 1134.0 nM 5.95
CHEMBL2152149 IC50 = 1186.0 nM 5.93
CHEMBL2152134 IC50 = 1202.0 nM 5.92
CHEMBL2152147 IC50 = 1253.0 nM 5.90
CHEMBL2152255 IC50 = 1316.0 nM 5.88
CHEMBL2152143 IC50 = 1355.0 nM 5.87
CHEMBL2152133 IC50 = 1418.0 nM 5.85
CHEMBL2152135 IC50 = 1582.0 nM 5.80
CHEMBL2152251 IC50 = 2452.0 nM 5.61
CHEMBL2152138 IC50 = 2964.0 nM 5.53
CHEMBL2152137 IC50 = 3389.0 nM 5.47
CHEMBL2152125 IC50 = 4204.0 nM 5.38
CHEMBL2152254 IC50 = 4389.0 nM 5.36
CHEMBL2152128 IC50 = 8359.0 nM 5.08