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Assay Detail

CHEMBL4709225

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

Functional
Reversal of multidrug resistance activity in P-gp overexpressing human KB-VIN cells assessed as potentiation of VCR-induced cytotoxicity by measuring VCR IC50 at 10 uM incubated for 48 hrs in presence of VCR by MTT assay (Rvb = 666.3 nM)
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type KB-VIN
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

New Seco-DSP derivatives as potent chemosensitizers.
Wan Q,Jin X,Guo Y,Yu Z,Guo S,Morris-Natschke S,Lee KH,Liu H,Chen Y
Eur J Med Chem (2020) 204 : 112555 -112555
PubMed 32750634 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 8.75 8.98

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4743412 1 8.98
CHEMBL4758059 1 8.97
CHEMBL4755219 1 8.96
CHEMBL4748813 1 8.94
CHEMBL4779274 1 8.85
CHEMBL4760012 1 8.80
CHEMBL4795629 1 8.80
CHEMBL6966 VERAPAMIL 4.0 1 8.80
CHEMBL4793184 1 8.71
CHEMBL4797081 1 8.71
CHEMBL4777677 1 8.65
CHEMBL4746188 1 8.57
CHEMBL4743006 1 8.55
CHEMBL4763859 1 8.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4743412 IC50 = 1.053 nM 8.98
CHEMBL4758059 IC50 = 1.061 nM 8.97
CHEMBL4755219 IC50 = 1.103 nM 8.96
CHEMBL4748813 IC50 = 1.151 nM 8.94
CHEMBL4779274 IC50 = 1.429 nM 8.85
CHEMBL4760012 IC50 = 1.57 nM 8.80
CHEMBL4795629 IC50 = 1.588 nM 8.80
CHEMBL6966 VERAPAMIL IC50 = 1.593 nM 8.80
CHEMBL4793184 IC50 = 1.942 nM 8.71
CHEMBL4797081 IC50 = 1.947 nM 8.71
CHEMBL4777677 IC50 = 2.228 nM 8.65
CHEMBL4746188 IC50 = 2.692 nM 8.57
CHEMBL4743006 IC50 = 2.842 nM 8.55
CHEMBL4763859 IC50 = 6.331 nM 8.20