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Assay Detail

CHEMBL692783

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Functional
In vitro inhibition of Bax regulated release of cytochrome C was determined using liposome channel assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HeLa
Confidence 1 — Organism
Curated By Intermediate

Target

HeLa (CHEMBL399)
Type CELL-LINE
Organism Homo sapiens

Publication

3,6-dibromocarbazole piperazine derivatives of 2-propanol as first inhibitors of cytochrome c release via Bax channel modulation.
Bombrun A, Gerber P, Casi G, Terradillos O, Antonsson B, Halazy S.
J Med Chem (2003) 46 : 4365 -4368
PubMed 14521400 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.28 7.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL139312 1 7.54
CHEMBL344483 1 6.43
CHEMBL334802 1 6.33
CHEMBL136513 1 6.32
CHEMBL343732 1 6.28
CHEMBL136947 1 6.17
CHEMBL136744 1 6.17
CHEMBL336890 1 6.02
CHEMBL344194 1 5.90
CHEMBL136725 1 5.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL139312 IC50 = 29.0 nM 7.54
CHEMBL344483 IC50 = 370.0 nM 6.43
CHEMBL334802 IC50 = 470.0 nM 6.33
CHEMBL136513 IC50 = 480.0 nM 6.32
CHEMBL343732 IC50 = 520.0 nM 6.28
CHEMBL136947 IC50 = 680.0 nM 6.17
CHEMBL136744 IC50 = 680.0 nM 6.17
CHEMBL336890 IC50 = 960.0 nM 6.02
CHEMBL344194 IC50 = 1270.0 nM 5.90
CHEMBL136725 IC50 = 2380.0 nM 5.62