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Assay Detail

CHEMBL999124

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Functional
Inhibition of TXB2 production in Sprague-Dawley rat whole blood
ChEMBL ↗
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Blood
Confidence 1 — Organism
Curated By Autocuration

Target

Blood (CHEMBL613615) ↗
Type TISSUE
Organism Rattus norvegicus

Publication

Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
McKew JC, Lee KL, Shen MW, Thakker P, Foley MA, Behnke ML, Hu B, Sum FW, Tam S, Hu Y, Chen L, Kirincich SJ, Michalak R, Thomason J, Ipek M, Wu K, Wooder L, Ramarao MK, Murphy EA, Goodwin DG, Albert L, Xu X, Donahue F, Ku MS, Keith J, Nickerson-Nutter CL, Abraham WM, Williams C, Hegen M, Clark JD.
J Med Chem (2008) 51 : 3388 -3413
PubMed 18498150 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 7.03 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL506470 — — 1 7.70
CHEMBL505164 — — 1 7.70
CHEMBL508521 — — 1 7.70
CHEMBL511076 — — 1 7.70
CHEMBL507809 — — 1 7.52
CHEMBL507093 — — 1 7.52
CHEMBL505012 — — 1 7.52
CHEMBL404529 — — 1 7.52
CHEMBL508679 — — 1 7.52
CHEMBL455228 — — 1 7.40
CHEMBL374878 — — 1 7.30
CHEMBL448357 — — 1 7.22
CHEMBL502125 — — 1 7.16
CHEMBL449293 — — 1 7.16
CHEMBL403734 — — 1 7.16
CHEMBL500889 — — 1 7.16
CHEMBL498953 — — 1 7.16
CHEMBL272342 EFIPLADIB 2.0 1 7.16
CHEMBL40014 — — 1 7.10
CHEMBL443459 — — 1 7.10
CHEMBL506787 — — 1 7.05
CHEMBL373778 — — 1 6.92
CHEMBL504502 — — 1 6.85
CHEMBL509063 — — 1 6.82
CHEMBL507662 — — 1 6.82
CHEMBL510703 — — 1 6.82
CHEMBL449770 — — 1 6.82
CHEMBL269787 ECOPLADIB 2.0 1 6.80
CHEMBL511036 — — 1 6.80
CHEMBL505917 — — 1 6.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL506470 — IC50 = 20.0 nM 7.70
CHEMBL511076 — IC50 = 20.0 nM 7.70
CHEMBL508521 — IC50 = 20.0 nM 7.70
CHEMBL505164 — IC50 = 20.0 nM 7.70
CHEMBL507809 — IC50 = 30.0 nM 7.52
CHEMBL507093 — IC50 = 30.0 nM 7.52
CHEMBL505012 — IC50 = 30.0 nM 7.52
CHEMBL404529 — IC50 = 30.0 nM 7.52
CHEMBL508679 — IC50 = 30.0 nM 7.52
CHEMBL455228 — IC50 = 40.0 nM 7.40
CHEMBL374878 — IC50 = 50.0 nM 7.30
CHEMBL448357 — IC50 = 60.0 nM 7.22
CHEMBL272342 EFIPLADIB IC50 = 70.0 nM 7.16
CHEMBL498953 — IC50 = 70.0 nM 7.16
CHEMBL500889 — IC50 = 70.0 nM 7.16
CHEMBL502125 — IC50 = 70.0 nM 7.16
CHEMBL403734 — IC50 = 70.0 nM 7.16
CHEMBL449293 — IC50 = 70.0 nM 7.16
CHEMBL443459 — IC50 = 80.0 nM 7.10
CHEMBL40014 — IC50 = 80.0 nM 7.10
CHEMBL506787 — IC50 = 90.0 nM 7.05
CHEMBL373778 — IC50 = 120.0 nM 6.92
CHEMBL504502 — IC50 = 140.0 nM 6.85
CHEMBL509063 — IC50 = 150.0 nM 6.82
CHEMBL507662 — IC50 = 150.0 nM 6.82
CHEMBL510703 — IC50 = 150.0 nM 6.82
CHEMBL449770 — IC50 = 150.0 nM 6.82
CHEMBL269787 ECOPLADIB IC50 = 160.0 nM 6.80
CHEMBL511036 — IC50 = 160.0 nM 6.80
CHEMBL505917 — IC50 = 340.0 nM 6.47
CHEMBL503543 — IC50 = 350.0 nM 6.46
CHEMBL506152 — IC50 = 360.0 nM 6.44
CHEMBL505534 — IC50 = 360.0 nM 6.44
CHEMBL506676 — IC50 = 400.0 nM 6.40
CHEMBL446030 — IC50 = 900.0 nM 6.05
CHEMBL498828 — IC50 = 1800.0 nM 5.75
CHEMBL473777 — IC50 > 10000.0 nM -
CHEMBL502920 — IC50 > 10000.0 nM -
CHEMBL506793 — IC50 - — -