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Assay Detail

CHEMBL5578036

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

Functional
Inhibition of cell proliferation in human KLE cells incubated for 48 hrs by CCK-8 assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

KLE (CHEMBL2366239)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of Novel Azaphenothiazine Derivatives to Suppress Endometrial Cancer by Targeting GRP75 to Impair Its Interaction with IP3R and Mitochondrial Ca<sup>2+</sup> Homeostasis.
Ling X, Zhang J, Song L, Wu H, Wang Q, Liu X, Ni W, Li J, Wang Y, Mao F.
J Med Chem (2024) 67 : 13829 -13851
PubMed 39082833 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.16 5.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5595115 1 5.54
CHEMBL5583884 1 5.50
CHEMBL5592860 1 5.50
CHEMBL5594405 1 5.46
CHEMBL5591081 1 5.45
CHEMBL5591987 1 5.40
CHEMBL5583814 1 5.21
CHEMBL5595504 1 5.09
CHEMBL5591231 1 5.08
CHEMBL5593982 1 5.07
CHEMBL5590735 1 5.02
CHEMBL5591062 1 5.00
CHEMBL5595359 1 4.99
CHEMBL5590484 1 4.97
CHEMBL5590128 1 4.84
CHEMBL1713 CHLORPROMAZINE HYDROCHLORIDE 4.0 1 4.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5595115 IC50 = 2880.0 nM 5.54
CHEMBL5583884 IC50 = 3170.0 nM 5.50
CHEMBL5592860 IC50 = 3180.0 nM 5.50
CHEMBL5594405 IC50 = 3490.0 nM 5.46
CHEMBL5591081 IC50 = 3530.0 nM 5.45
CHEMBL5591987 IC50 = 3960.0 nM 5.40
CHEMBL5583814 IC50 = 6230.0 nM 5.21
CHEMBL5595504 IC50 = 8060.0 nM 5.09
CHEMBL5591231 IC50 = 8310.0 nM 5.08
CHEMBL5593982 IC50 = 8520.0 nM 5.07
CHEMBL5590735 IC50 = 9550.0 nM 5.02
CHEMBL5591062 IC50 = 9990.0 nM 5.00
CHEMBL5595359 IC50 = 10320.0 nM 4.99
CHEMBL5590484 IC50 = 10740.0 nM 4.97
CHEMBL5590128 IC50 = 14450.0 nM 4.84
CHEMBL1713 CHLORPROMAZINE HYDROCHLORIDE IC50 = 35010.0 nM 4.46