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Assay Detail

CHEMBL4045586

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

Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Identification of pyrazolopyrimidine arylsulfonamides as CC-chemokine receptor 4 (CCR4) antagonists.
Miah AH, Champigny AC, Graves RH, Hodgson ST, Percy JM, Procopiou PA.
Bioorg Med Chem (2017) 25 : 5327 -5340
PubMed 28801066 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 6.22 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2018954 1 8.41
CHEMBL2018953 1 8.26
CHEMBL4060413 1 7.20
CHEMBL4071299 1 7.10
CHEMBL4069639 1 7.10
CHEMBL4069103 1 6.80
CHEMBL4088207 1 6.70
CHEMBL4080352 1 6.60
CHEMBL4096860 1 6.60
CHEMBL4098813 1 6.60
CHEMBL4068045 1 6.50
CHEMBL4089151 1 6.50
CHEMBL4071815 1 6.30
CHEMBL3310825 1 6.22
CHEMBL4093509 1 6.20
CHEMBL4095437 1 6.20
CHEMBL4066934 1 6.20
CHEMBL4091069 1 6.10
CHEMBL4060967 1 6.10
CHEMBL4082318 1 6.10
CHEMBL4067451 1 6.10
CHEMBL4093994 1 5.90
CHEMBL4097341 1 5.70
CHEMBL4078359 1 5.50
CHEMBL4065904 1 5.50
CHEMBL4104585 1 5.40
CHEMBL4059913 1 5.10
CHEMBL4088688 1 5.00
CHEMBL4098333 1 5.00
CHEMBL4066451 1 4.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2018954 IC50 = 3.89 nM 8.41
CHEMBL2018953 IC50 = 5.495 nM 8.26
CHEMBL4060413 IC50 = 63.1 nM 7.20
CHEMBL4071299 IC50 = 79.43 nM 7.10
CHEMBL4069639 IC50 = 79.43 nM 7.10
CHEMBL4069103 IC50 = 158.49 nM 6.80
CHEMBL4088207 IC50 = 199.53 nM 6.70
CHEMBL4080352 IC50 = 251.19 nM 6.60
CHEMBL4096860 IC50 = 251.19 nM 6.60
CHEMBL4098813 IC50 = 251.19 nM 6.60
CHEMBL4068045 IC50 = 316.23 nM 6.50
CHEMBL4089151 IC50 = 316.23 nM 6.50
CHEMBL4071815 IC50 = 501.19 nM 6.30
CHEMBL3310825 IC50 = 602.56 nM 6.22
CHEMBL4095437 IC50 = 630.96 nM 6.20
CHEMBL4066934 IC50 = 630.96 nM 6.20
CHEMBL4093509 IC50 = 630.96 nM 6.20
CHEMBL4091069 IC50 = 794.33 nM 6.10
CHEMBL4060967 IC50 = 794.33 nM 6.10
CHEMBL4082318 IC50 = 794.33 nM 6.10
CHEMBL4067451 IC50 = 794.33 nM 6.10
CHEMBL4093994 IC50 = 1258.93 nM 5.90
CHEMBL4097341 IC50 = 1995.26 nM 5.70
CHEMBL4065904 IC50 = 3162.28 nM 5.50
CHEMBL4078359 IC50 = 3162.28 nM 5.50
CHEMBL4104585 IC50 = 3981.07 nM 5.40
CHEMBL4059913 IC50 = 7943.28 nM 5.10
CHEMBL4088688 IC50 = 10000.0 nM 5.00
CHEMBL4098333 IC50 = 10000.0 nM 5.00
CHEMBL4066451 IC50 = 12589.25 nM 4.90
CHEMBL4090166 IC50 = 15848.93 nM 4.80
CHEMBL4063189 IC50 > 31622.78 nM -
CHEMBL4081830 IC50 > 31622.78 nM -