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Assay Detail

CHEMBL2339990

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

Binding
Inhibition of ACAT1 (unknown origin) expressed in CHO cells
ChEMBL ↗
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sterol O-acyltransferase 1 (CHEMBL2782) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationship of pyripyropene A derivatives as potent and selective acyl-CoA:cholesterol acyltransferase 2 (ACAT2) inhibitors: part 1.
Ohtawa M, Yamazaki H, Ohte S, Matsuda D, Ohshiro T, Rudel LL, Omura S, Tomoda H, Nagamitsu T.
Bioorg Med Chem Lett (2013) 23 : 1285 -1287
PubMed 23369538 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 44 6.13 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2334201 — — 1 6.96
CHEMBL2333809 — — 1 6.92
CHEMBL2334204 — — 1 6.82
CHEMBL2334205 — — 1 6.82
CHEMBL2334198 — — 1 6.72
CHEMBL2333808 — — 1 6.72
CHEMBL2334200 — — 1 6.68
CHEMBL2334540 — — 1 6.64
CHEMBL2334197 — — 1 6.60
CHEMBL2334222 — — 1 6.57
CHEMBL2334203 — — 1 6.38
CHEMBL2334215 — — 1 6.37
CHEMBL2334224 — — 1 6.34
CHEMBL2334212 — — 1 6.31
CHEMBL2334538 — — 1 6.29
CHEMBL2333812 — — 1 6.27
CHEMBL2334196 — — 1 6.19
CHEMBL2334217 — — 1 6.19
CHEMBL2334199 — — 1 6.18
CHEMBL2334220 — — 1 6.17
CHEMBL2334221 — — 1 6.16
CHEMBL2334541 — — 1 6.16
CHEMBL2334223 — — 1 6.15
CHEMBL2334195 — — 1 6.15
CHEMBL2333810 — — 1 6.10
CHEMBL2333811 — — 1 6.08
CHEMBL2334219 — — 1 6.05
CHEMBL2334214 — — 1 6.02
CHEMBL2334206 — — 1 6.00
CHEMBL2334207 — — 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2334201 — IC50 = 110.0 nM 6.96
CHEMBL2333809 — IC50 = 120.0 nM 6.92
CHEMBL2334205 — IC50 = 150.0 nM 6.82
CHEMBL2334204 — IC50 = 150.0 nM 6.82
CHEMBL2334198 — IC50 = 190.0 nM 6.72
CHEMBL2333808 — IC50 = 190.0 nM 6.72
CHEMBL2334200 — IC50 = 210.0 nM 6.68
CHEMBL2334540 — IC50 = 230.0 nM 6.64
CHEMBL2334197 — IC50 = 250.0 nM 6.60
CHEMBL2334222 — IC50 = 270.0 nM 6.57
CHEMBL2334203 — IC50 = 420.0 nM 6.38
CHEMBL2334215 — IC50 = 430.0 nM 6.37
CHEMBL2334224 — IC50 = 460.0 nM 6.34
CHEMBL2334212 — IC50 = 490.0 nM 6.31
CHEMBL2334538 — IC50 = 510.0 nM 6.29
CHEMBL2333812 — IC50 = 540.0 nM 6.27
CHEMBL2334196 — IC50 = 650.0 nM 6.19
CHEMBL2334217 — IC50 = 650.0 nM 6.19
CHEMBL2334199 — IC50 = 660.0 nM 6.18
CHEMBL2334220 — IC50 = 680.0 nM 6.17
CHEMBL2334221 — IC50 = 700.0 nM 6.16
CHEMBL2334541 — IC50 = 690.0 nM 6.16
CHEMBL2334223 — IC50 = 710.0 nM 6.15
CHEMBL2334195 — IC50 = 710.0 nM 6.15
CHEMBL2333810 — IC50 = 790.0 nM 6.10
CHEMBL2333811 — IC50 = 830.0 nM 6.08
CHEMBL2334219 — IC50 = 890.0 nM 6.05
CHEMBL2334214 — IC50 = 960.0 nM 6.02
CHEMBL2334206 — IC50 = 1000.0 nM 6.00
CHEMBL2334207 — IC50 = 1000.0 nM 6.00
CHEMBL2334216 — IC50 = 1150.0 nM 5.94
CHEMBL2333813 — IC50 = 1170.0 nM 5.93
CHEMBL2334218 — IC50 = 1430.0 nM 5.84
CHEMBL2334210 — IC50 = 1620.0 nM 5.79
CHEMBL2334202 — IC50 = 2230.0 nM 5.65
CHEMBL2334209 — IC50 = 2690.0 nM 5.57
CHEMBL2334211 — IC50 = 2800.0 nM 5.55
CHEMBL2334536 — IC50 = 3200.0 nM 5.50
CHEMBL2334537 — IC50 = 3800.0 nM 5.42
CHEMBL2334213 — IC50 = 4140.0 nM 5.38
CHEMBL2334539 — IC50 = 4160.0 nM 5.38
CHEMBL2334208 — IC50 = 5100.0 nM 5.29
CHEMBL2334194 — IC50 = 7410.0 nM 5.13
CHEMBL179229 PYRIPYROPENE A IC50 > 80000.0 nM -