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Assay Detail

CHEMBL4124699

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ADMET
Cytotoxicity against rat bone marrow cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Rattus norvegicus
Cell Type Bone marrow cell
Confidence 1 — Organism
Curated By Intermediate

Publication

Small Molecule Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitors: Hit to Lead Optimization of Systemic Agents.
Londregan AT, Wei L, Xiao J, Lintner NG, Petersen D, Dullea RG, McClure KF, Bolt MW, Warmus JS, Coffey SB, Limberakis C, Genovino J, Thuma BA, Hesp KD, Aspnes GE, Reidich B, Salatto CT, Chabot JR, Cate JHD, Liras S, Piotrowski DW.
J Med Chem (2018) 61 : 5704 -5718
PubMed 29878763 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.27 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4126496 1 6.00
CHEMBL4109308 1 5.92
CHEMBL4130157 1 5.85
CHEMBL4128388 1 5.54
CHEMBL4126072 1 4.71
CHEMBL4127311 1 4.52
CHEMBL4127458 1 4.36
CHEMBL4128250 1 -
CHEMBL4127016 1 -
CHEMBL3952343 1 -
CHEMBL4114159 1 -
CHEMBL4108338 1 -
CHEMBL4107559 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4126496 IC50 = 1000.0 nM 6.00
CHEMBL4109308 IC50 = 1200.0 nM 5.92
CHEMBL4130157 IC50 = 1400.0 nM 5.85
CHEMBL4128388 IC50 = 2900.0 nM 5.54
CHEMBL4126072 IC50 = 19600.0 nM 4.71
CHEMBL4127311 IC50 = 30100.0 nM 4.52
CHEMBL4127458 IC50 = 43700.0 nM 4.36
CHEMBL4128250 IC50 > 20000.0 nM -
CHEMBL4127016 IC50 > 20000.0 nM -
CHEMBL3952343 IC50 > 20000.0 nM -
CHEMBL4114159 IC50 > 19700.0 nM -
CHEMBL4108338 IC50 > 12700.0 nM -
CHEMBL4107559 IC50 >= 20000.0 nM -