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Assay Detail

CHEMBL3367642

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

Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

C-C chemokine receptor type 4 (CHEMBL2414)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Lead identification of benzimidazolone and azabenzimidazolone arylsulfonamides as CC-chemokine receptor 4 (CCR4) antagonists.
Miah AH, Abas H, Begg M, Marsh BJ, O'Flynn DE, Ford AJ, Percy JM, Procopiou PA, Richards SA, Rumley SA.
Bioorg Med Chem (2014) 22 : 4298 -4311
PubMed 24909677 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.54 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2018954 1 8.41
CHEMBL2018953 1 8.26
CHEMBL3310839 1 7.60
CHEMBL3310841 1 7.30
CHEMBL3310840 1 7.10
CHEMBL3310833 1 6.95
CHEMBL3310827 1 6.70
CHEMBL3310838 1 6.70
CHEMBL3310826 1 6.50
CHEMBL3310837 1 6.40
CHEMBL3310830 1 6.34
CHEMBL3310825 1 6.22
CHEMBL3310832 1 6.00
CHEMBL3310836 1 5.80
CHEMBL3310829 1 5.70
CHEMBL3310835 1 5.70
CHEMBL3310834 1 5.40
CHEMBL3310828 1 4.70
CHEMBL3310831 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2018954 IC50 = 3.89 nM 8.41
CHEMBL2018953 IC50 = 5.495 nM 8.26
CHEMBL3310839 IC50 = 25.12 nM 7.60
CHEMBL3310841 IC50 = 50.12 nM 7.30
CHEMBL3310840 IC50 = 79.43 nM 7.10
CHEMBL3310833 IC50 = 112.2 nM 6.95
CHEMBL3310827 IC50 = 199.53 nM 6.70
CHEMBL3310838 IC50 = 199.53 nM 6.70
CHEMBL3310826 IC50 = 316.23 nM 6.50
CHEMBL3310837 IC50 = 398.11 nM 6.40
CHEMBL3310830 IC50 = 457.09 nM 6.34
CHEMBL3310825 IC50 = 602.56 nM 6.22
CHEMBL3310832 IC50 = 1000.0 nM 6.00
CHEMBL3310836 IC50 = 1584.89 nM 5.80
CHEMBL3310829 IC50 = 1995.26 nM 5.70
CHEMBL3310835 IC50 = 1995.26 nM 5.70
CHEMBL3310834 IC50 = 3981.07 nM 5.40
CHEMBL3310828 IC50 = 19952.62 nM 4.70
CHEMBL3310831 IC50 > 31622.78 nM -