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Assay Detail

CHEMBL5365870

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

Toxicity
Cytotoxicity against rat Bone marrow cell assessed as inhibition of cell growth with (R)-4-(3H-[1,2,3]triazolo[4,5-b]pyridin-3-yl)-N-(3-chloropyridin-2-yl)-N-(piperidin-3-yl) benzamide as high potent effect standard by celltiter-glo assay
34
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Toxicity
Organism Rattus norvegicus
Cell Type Bone marrow cell
Confidence 1 — Organism
Curated By Autocuration

Publication

Small molecule inhibitors of PCSK9. SAR investigations of head and amine groups.
Aspnes GE, Coffey SB, Darout E, Dechert-Schmitt AM, Dullea RG, Kamlet AS, Limberakis C, Londregan AT, McClure KF, Menhaji-Klotz E, Piotrowski DW, Polivkova J, Raymer B, Ruggeri RB, Salatto CT, Tu M, Wei L, Xiao J.
Bioorg Med Chem Lett (2023) 92 : 129394 -129394
PubMed 37379958 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 4.79 5.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4109308 1 5.49
CHEMBL5436376 1 5.19
CHEMBL5397401 2 5.14
CHEMBL5394025 1 4.96
CHEMBL5408894 1 4.90
CHEMBL5408632 1 4.86
CHEMBL4107804 1 4.74
CHEMBL5401016 1 4.67
CHEMBL5398982 2 4.66
CHEMBL5417992 2 4.63
CHEMBL4107559 1 4.57
CHEMBL5406351 1 4.12
CHEMBL5414767 1 -
CHEMBL5440847 1 -
CHEMBL5415107 1 -
CHEMBL5427421 1 -
CHEMBL5414978 1 -
CHEMBL5407175 1 -
CHEMBL5433750 1 -
CHEMBL5431139 1 -
CHEMBL5421898 1 -
CHEMBL5400549 1 -
CHEMBL5405461 1 -
CHEMBL5406095 1 -
CHEMBL5414972 1 -
CHEMBL5420031 1 -
CHEMBL5418395 1 -
CHEMBL5403764 1 -
CHEMBL5414993 1 -
CHEMBL5403420 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4109308 IC50 = 3230.0 nM 5.49
CHEMBL5436376 IC50 = 6440.0 nM 5.19
CHEMBL5397401 IC50 = 7200.0 nM 5.14
CHEMBL5397401 IC50 = 9900.0 nM 5.00
CHEMBL5394025 IC50 = 10920.0 nM 4.96
CHEMBL5408894 IC50 = 12500.0 nM 4.90
CHEMBL5408632 IC50 = 13750.0 nM 4.86
CHEMBL4107804 IC50 = 18230.0 nM 4.74
CHEMBL5401016 IC50 = 21210.0 nM 4.67
CHEMBL5398982 IC50 = 22000.0 nM 4.66
CHEMBL5417992 IC50 = 23300.0 nM 4.63
CHEMBL4107559 IC50 = 27060.0 nM 4.57
CHEMBL5417992 IC50 = 35600.0 nM 4.45
CHEMBL5398982 IC50 = 37200.0 nM 4.43
CHEMBL5406351 IC50 = 76600.0 nM 4.12
CHEMBL5406095 IC50 - -
CHEMBL5400549 IC50 - -
CHEMBL5403420 IC50 - -
CHEMBL5431139 IC50 - -
CHEMBL5415107 IC50 - -
CHEMBL5414787 IC50 - -
CHEMBL5421898 IC50 - -
CHEMBL5414767 IC50 - -
CHEMBL5440847 IC50 - -
CHEMBL5427421 IC50 - -
CHEMBL5414978 IC50 - -
CHEMBL5407175 IC50 - -
CHEMBL5433750 IC50 - -
CHEMBL5414993 IC50 - -
CHEMBL5403764 IC50 - -
CHEMBL5418395 IC50 - -
CHEMBL5420031 IC50 - -
CHEMBL5405461 IC50 > 100000.0 nM -
CHEMBL5414972 IC50 - -