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Assay Detail

CHEMBL947342

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Binding
Inhibition of human cytosolic PLA2alpha by GLU micelle assay
ChEMBL ↗
65
Total Activities
65
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

Cytosolic phospholipase A2 (CHEMBL3816) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Reactions of functionalized sulfonamides: application to lowering the lipophilicity of cytosolic phospholipase A2alpha inhibitors.
Chen L, Wang W, Lee KL, Shen MW, Murphy EA, Zhang W, Xu X, Tam S, Nickerson-Nutter C, Goodwin DG, Clark JD, McKew JC.
J Med Chem (2009) 52 : 1156 -1171
PubMed 19178292 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 65 6.73 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL451642 — — 1 8.22
CHEMBL507864 — — 1 8.00
CHEMBL404529 — — 1 8.00
CHEMBL504617 — — 1 7.89
CHEMBL505593 — — 1 7.70
CHEMBL506097 — — 1 7.66
CHEMBL505164 — — 1 7.58
CHEMBL504746 — — 1 7.52
CHEMBL272342 EFIPLADIB 2.0 1 7.40
CHEMBL503626 — — 1 7.00
CHEMBL408261 — — 1 7.00
CHEMBL373778 — — 1 6.96
CHEMBL501852 — — 1 6.92
CHEMBL504728 — — 1 6.89
CHEMBL455363 — — 1 6.85
CHEMBL269787 ECOPLADIB 2.0 1 6.82
CHEMBL448596 — — 1 6.82
CHEMBL448664 — — 1 6.82
CHEMBL449113 — — 1 6.82
CHEMBL503141 — — 1 6.77
CHEMBL501496 — — 1 6.77
CHEMBL510044 — — 1 6.75
CHEMBL453714 — — 1 6.72
CHEMBL504280 — — 1 6.70
CHEMBL468377 — — 1 6.70
CHEMBL499284 — — 1 6.70
CHEMBL501336 — — 1 6.70
CHEMBL510703 — — 1 6.70
CHEMBL504730 — — 1 6.66
CHEMBL447045 — — 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL451642 — IC50 = 6.0 nM 8.22
CHEMBL507864 — IC50 = 10.0 nM 8.00
CHEMBL404529 — IC50 = 10.0 nM 8.00
CHEMBL504617 — IC50 = 13.0 nM 7.89
CHEMBL505593 — IC50 = 20.0 nM 7.70
CHEMBL506097 — IC50 = 22.0 nM 7.66
CHEMBL505164 — IC50 = 26.0 nM 7.58
CHEMBL504746 — IC50 = 30.0 nM 7.52
CHEMBL272342 EFIPLADIB IC50 = 40.0 nM 7.40
CHEMBL503626 — IC50 = 100.0 nM 7.00
CHEMBL408261 — IC50 = 100.0 nM 7.00
CHEMBL373778 — IC50 = 110.0 nM 6.96
CHEMBL501852 — IC50 = 120.0 nM 6.92
CHEMBL504728 — IC50 = 130.0 nM 6.89
CHEMBL455363 — IC50 = 140.0 nM 6.85
CHEMBL269787 ECOPLADIB IC50 = 150.0 nM 6.82
CHEMBL449113 — IC50 = 150.0 nM 6.82
CHEMBL448664 — IC50 = 150.0 nM 6.82
CHEMBL448596 — IC50 = 150.0 nM 6.82
CHEMBL503141 — IC50 = 170.0 nM 6.77
CHEMBL501496 — IC50 = 170.0 nM 6.77
CHEMBL510044 — IC50 = 180.0 nM 6.75
CHEMBL453714 — IC50 = 190.0 nM 6.72
CHEMBL510703 — IC50 = 200.0 nM 6.70
CHEMBL501336 — IC50 = 200.0 nM 6.70
CHEMBL499284 — IC50 = 200.0 nM 6.70
CHEMBL504280 — IC50 = 200.0 nM 6.70
CHEMBL468377 — IC50 = 200.0 nM 6.70
CHEMBL504730 — IC50 = 220.0 nM 6.66
CHEMBL447045 — IC50 = 220.0 nM 6.66
CHEMBL449829 — IC50 = 240.0 nM 6.62
CHEMBL444909 — IC50 = 250.0 nM 6.60
CHEMBL488320 — IC50 = 250.0 nM 6.60
CHEMBL455572 — IC50 = 250.0 nM 6.60
CHEMBL449856 — IC50 = 270.0 nM 6.57
CHEMBL443645 — IC50 = 270.0 nM 6.57
CHEMBL501774 — IC50 = 290.0 nM 6.54
CHEMBL504084 — IC50 = 300.0 nM 6.52
CHEMBL503893 — IC50 = 300.0 nM 6.52
CHEMBL503263 — IC50 = 320.0 nM 6.50
CHEMBL502458 — IC50 = 330.0 nM 6.48
CHEMBL502901 — IC50 = 330.0 nM 6.48
CHEMBL468442 — IC50 = 330.0 nM 6.48
CHEMBL506138 — IC50 = 350.0 nM 6.46
CHEMBL448639 — IC50 = 350.0 nM 6.46
CHEMBL509488 — IC50 = 350.0 nM 6.46
CHEMBL474478 — IC50 = 350.0 nM 6.46
CHEMBL504199 — IC50 = 360.0 nM 6.44
CHEMBL510461 — IC50 = 380.0 nM 6.42
CHEMBL451133 — IC50 = 390.0 nM 6.41