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Assay Detail

CHEMBL641708

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Binding
In vitro inhibitory activity against acyl coenzyme A:cholesterol acyltransferase 1 of liver microsomes isolated from cholesterol-fed rats.
ChEMBL ↗
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Liver
Confidence 9 — Direct single protein target
Curated By Expert

Target

Sterol O-acyltransferase 1 (CHEMBL285) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Inhibitors of acyl-CoA:cholesterol O-acyltransferase. synthesis and pharmacological activity of (+/-)-2-dodecyl-alpha-phenyl-N-(2,4,6-trimethoxyphenyl)-2H-tetrazole-5- acetamide and structurally related tetrazole amide derivatives.
O'Brien PM, Sliskovic DR, Picard JA, Lee HT, Purchase CF, Roth BD, White AD, Anderson M, Mueller SB, Bocan T, Bousley R, Hamelehle KL, Homan R, Lee P, Krause BR, Reindel JF, Stanfield RL, Turluck D.
J Med Chem (1996) 39 : 2354 -2366
PubMed 8691430 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 6.94 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL264861 — — 1 8.30
CHEMBL175982 — — 1 8.22
CHEMBL306344 — — 1 8.00
CHEMBL310568 — — 1 7.89
CHEMBL78038 — — 1 7.89
CHEMBL80270 — — 1 7.82
CHEMBL77653 — — 1 7.68
CHEMBL77370 — — 1 7.64
CHEMBL77512 — — 1 7.62
CHEMBL76922 — — 1 7.60
CHEMBL78106 — — 1 7.58
CHEMBL80923 — — 1 7.55
CHEMBL77319 — — 1 7.52
CHEMBL76919 — — 1 7.51
CHEMBL78270 — — 1 7.51
CHEMBL77087 — — 1 7.48
CHEMBL76481 — — 1 7.44
CHEMBL77467 — — 1 7.28
CHEMBL76950 — — 1 7.27
CHEMBL80580 — — 1 7.25
CHEMBL421315 — — 1 7.20
CHEMBL78155 — — 1 7.07
CHEMBL305912 — — 1 6.70
CHEMBL80398 — — 1 6.66
CHEMBL80781 — — 1 6.61
CHEMBL77496 — — 1 6.57
CHEMBL310637 — — 1 6.32
CHEMBL76720 — — 1 6.32
CHEMBL80870 — — 1 6.32
CHEMBL76034 — — 1 6.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL264861 — IC50 = 5.0 nM 8.30
CHEMBL175982 — IC50 = 6.0 nM 8.22
CHEMBL306344 — IC50 = 10.0 nM 8.00
CHEMBL310568 — IC50 = 13.0 nM 7.89
CHEMBL78038 — IC50 = 13.0 nM 7.89
CHEMBL80270 — IC50 = 15.0 nM 7.82
CHEMBL77653 — IC50 = 21.0 nM 7.68
CHEMBL77370 — IC50 = 23.0 nM 7.64
CHEMBL77512 — IC50 = 24.0 nM 7.62
CHEMBL76922 — IC50 = 25.0 nM 7.60
CHEMBL78106 — IC50 = 26.0 nM 7.58
CHEMBL80923 — IC50 = 28.0 nM 7.55
CHEMBL77319 — IC50 = 30.0 nM 7.52
CHEMBL76919 — IC50 = 31.0 nM 7.51
CHEMBL78270 — IC50 = 31.0 nM 7.51
CHEMBL77087 — IC50 = 33.0 nM 7.48
CHEMBL76481 — IC50 = 36.0 nM 7.44
CHEMBL77467 — IC50 = 53.0 nM 7.28
CHEMBL76950 — IC50 = 54.0 nM 7.27
CHEMBL80580 — IC50 = 56.0 nM 7.25
CHEMBL421315 — IC50 = 63.0 nM 7.20
CHEMBL78155 — IC50 = 85.0 nM 7.07
CHEMBL305912 — IC50 = 200.0 nM 6.70
CHEMBL80398 — IC50 = 221.0 nM 6.66
CHEMBL80781 — IC50 = 244.0 nM 6.61
CHEMBL77496 — IC50 = 270.0 nM 6.57
CHEMBL310637 — IC50 = 480.0 nM 6.32
CHEMBL76720 — IC50 = 480.0 nM 6.32
CHEMBL80870 — IC50 = 480.0 nM 6.32
CHEMBL76034 — IC50 = 490.0 nM 6.31
CHEMBL77309 — IC50 = 590.0 nM 6.23
CHEMBL76092 — IC50 = 659.0 nM 6.18
CHEMBL80687 — IC50 = 1057.0 nM 5.98
CHEMBL75694 — IC50 = 1537.0 nM 5.81
CHEMBL76535 — IC50 = 1760.0 nM 5.75
CHEMBL76978 — IC50 = 3346.0 nM 5.47
CHEMBL76534 — IC50 = 13600.0 nM 4.87
CHEMBL78291 — IC50 = 35580.0 nM 4.45
CHEMBL76425 — IC50 > 5000.0 nM -
CHEMBL77474 — IC50 > 5000.0 nM -