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Assay Detail

CHEMBL5365558

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

Binding
Inhibition of ABCG2 (unknown origin)-mediated mitoxantrone efflux
25
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Inhibitors of ABCG2-mediated multidrug resistance: Lead generation through computer-aided drug design.
Goracci L, Nurisso A, Roussel E, Pérès B, Chaptal V, Falson P, Marminon C, Jose J, Le Borgne M, Boumendjel A.
Eur J Med Chem (2023) 248 : 115070 -115070
PubMed 36628850 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 25 6.30 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL488910 1 7.30
CHEMBL3110289 1 7.00
CHEMBL2011288 1 6.89
CHEMBL3353414 1 6.64
CHEMBL3110290 1 6.52
CHEMBL3353417 1 6.51
CHEMBL1957192 1 6.37
CHEMBL5402034 1 6.37
CHEMBL3110299 1 6.31
CHEMBL3353415 1 6.31
CHEMBL3353422 1 6.21
CHEMBL1957193 1 6.10
CHEMBL5433560 1 6.08
CHEMBL3110292 1 6.02
CHEMBL1957202 1 6.02
CHEMBL3108796 1 6.00
CHEMBL3110301 2 5.96
CHEMBL3110291 1 5.96
CHEMBL410316 FUMITREMORGIN 1 5.70
CHEMBL5426744 1 -
CHEMBL2436171 1 -
CHEMBL5414883 1 -
CHEMBL5434596 1 -
CHEMBL5435211 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL488910 EC50 = 50.0 nM 7.30
CHEMBL3110289 EC50 = 100.0 nM 7.00
CHEMBL2011288 EC50 = 130.0 nM 6.89
CHEMBL3353414 EC50 = 230.0 nM 6.64
CHEMBL3110290 EC50 = 300.0 nM 6.52
CHEMBL3353417 EC50 = 310.0 nM 6.51
CHEMBL1957192 EC50 = 430.0 nM 6.37
CHEMBL5402034 EC50 = 430.0 nM 6.37
CHEMBL3110299 EC50 = 490.0 nM 6.31
CHEMBL3353415 EC50 = 490.0 nM 6.31
CHEMBL3353422 EC50 = 610.0 nM 6.21
CHEMBL1957193 EC50 = 790.0 nM 6.10
CHEMBL5433560 EC50 = 840.0 nM 6.08
CHEMBL1957202 EC50 = 960.0 nM 6.02
CHEMBL3110292 EC50 = 960.0 nM 6.02
CHEMBL3108796 EC50 = 1000.0 nM 6.00
CHEMBL3110301 EC50 = 1100.0 nM 5.96
CHEMBL3110291 EC50 = 1110.0 nM 5.96
CHEMBL3110301 EC50 = 1800.0 nM 5.75
CHEMBL410316 FUMITREMORGIN EC50 = 2000.0 nM 5.70
CHEMBL5435211 EC50 - -
CHEMBL5434596 EC50 - -
CHEMBL5414883 EC50 - -
CHEMBL2436171 EC50 - -
CHEMBL5426744 EC50 - -