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Assay Detail

CHEMBL2019171

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

Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
20
Total Activities
20
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Lead optimisation of the N1 substituent of a novel series of indazole arylsulfonamides as CCR4 antagonists and identification of a candidate for clinical investigation.
Procopiou PA, Ford AJ, Graves RH, Hall DA, Hodgson ST, Lacroix YM, Needham D, Slack RJ.
Bioorg Med Chem Lett (2012) 22 : 2730 -2733
PubMed 22437117 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 7.31 9.10
pKi 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2018953 1 9.10
CHEMBL2018954 1 8.50
CHEMBL2018968 1 8.10
CHEMBL2018969 1 8.00
CHEMBL2018964 1 7.90
CHEMBL2018967 1 7.80
CHEMBL2018959 1 7.70
CHEMBL2018951 1 7.40
CHEMBL2018952 1 7.40
CHEMBL2016602 1 7.30
CHEMBL2018961 1 7.00
CHEMBL2018957 1 6.90
CHEMBL2018966 1 6.80
CHEMBL2018956 1 6.80
CHEMBL2018958 1 6.60
CHEMBL2018960 1 6.60
CHEMBL2018955 1 6.60
CHEMBL2018962 1 6.50
CHEMBL2018963 1 5.90
CHEMBL2018965 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2018953 Ki = 0.7943 nM 9.10
CHEMBL2018954 Ki = 3.162 nM 8.50
CHEMBL2018968 Ki = 7.943 nM 8.10
CHEMBL2018969 Ki = 10.0 nM 8.00
CHEMBL2018964 Ki = 12.59 nM 7.90
CHEMBL2018967 Ki = 15.85 nM 7.80
CHEMBL2018959 Ki = 19.95 nM 7.70
CHEMBL2018951 Ki = 39.81 nM 7.40
CHEMBL2018952 Ki = 39.81 nM 7.40
CHEMBL2016602 Ki = 50.12 nM 7.30
CHEMBL2018961 Ki = 100.0 nM 7.00
CHEMBL2018957 Ki = 125.89 nM 6.90
CHEMBL2018966 Ki = 158.49 nM 6.80
CHEMBL2018956 Ki = 158.49 nM 6.80
CHEMBL2018958 Ki = 251.19 nM 6.60
CHEMBL2018960 Ki = 251.19 nM 6.60
CHEMBL2018955 Ki = 251.19 nM 6.60
CHEMBL2018962 Ki = 316.23 nM 6.50
CHEMBL2018963 Ki = 1258.93 nM 5.90
CHEMBL2018965 pKi - -