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Assay Detail

CHEMBL3363219

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Functional
Induction of ABCA1 transcriptional activity in ABCA1p-LUC human HepG2 cells assessed as luciferase activity after 18 hrs
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HepG2
Confidence 1 — Organism
Curated By Autocuration

Target

HepG2 (CHEMBL395)
Type CELL-LINE
Organism Homo sapiens

Publication

Optimization of Rutaecarpine as ABCA1 Up-Regulator for Treating Atherosclerosis.
Li Y, Feng T, Liu P, Liu C, Wang X, Li D, Li N, Chen M, Xu Y, Si S.
ACS Med Chem Lett (2014) 5 : 884 -888
PubMed 25147608 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 5.71 7.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3326367 1 7.46
CHEMBL1927538 1 6.92
CHEMBL1512476 1 6.68
CHEMBL552178 1 6.15
CHEMBL3326362 1 6.09
CHEMBL3326385 1 5.89
CHEMBL3326387 1 5.81
CHEMBL3326365 1 5.78
CHEMBL3326366 1 5.48
CHEMBL1491339 NICOTREDOLE 2.0 1 5.43
CHEMBL3326390 1 5.20
CHEMBL3326364 1 5.18
CHEMBL3326389 1 5.05
CHEMBL3326363 1 4.97
CHEMBL3326388 1 4.71
CHEMBL3326386 1 4.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3326367 EC50 = 35.0 nM 7.46
CHEMBL1927538 EC50 = 121.0 nM 6.92
CHEMBL1512476 EC50 = 210.0 nM 6.68
CHEMBL552178 EC50 = 710.0 nM 6.15
CHEMBL3326362 EC50 = 810.0 nM 6.09
CHEMBL3326385 EC50 = 1280.0 nM 5.89
CHEMBL3326387 EC50 = 1560.0 nM 5.81
CHEMBL3326365 EC50 = 1660.0 nM 5.78
CHEMBL3326366 EC50 = 3280.0 nM 5.48
CHEMBL1491339 NICOTREDOLE EC50 = 3670.0 nM 5.43
CHEMBL3326390 EC50 = 6380.0 nM 5.20
CHEMBL3326364 EC50 = 6550.0 nM 5.18
CHEMBL3326389 EC50 = 8860.0 nM 5.05
CHEMBL3326363 EC50 = 10720.0 nM 4.97
CHEMBL3326388 EC50 = 19550.0 nM 4.71
CHEMBL3326386 EC50 = 33240.0 nM 4.48