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Assay Detail

CHEMBL4134307

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

Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
50
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of AZD-2098 and AZD-1678, Two Potent and Bioavailable CCR4 Receptor Antagonists.
Kindon N, Andrews G, Baxter A, Cheshire D, Hemsley P, Johnson T, Liu YZ, McGinnity D, McHale M, Mete A, Reuberson J, Roberts B, Steele J, Teobald B, Unitt J, Vaughan D, Walters I, Stocks MJ.
ACS Med Chem Lett (2017) 8 : 981 -986
PubMed 28947948 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 50 7.13 9.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4172769 1 9.50
CHEMBL4167445 1 9.20
CHEMBL4162364 1 9.00
CHEMBL4172635 1 8.60
CHEMBL4160218 1 8.60
CHEMBL4175323 1 8.40
CHEMBL4173046 1 8.40
CHEMBL4160846 1 8.40
CHEMBL4173861 1 8.10
CHEMBL4165356 1 8.10
CHEMBL4170431 1 8.00
CHEMBL4162097 1 7.90
CHEMBL4175972 1 7.90
CHEMBL4165939 1 7.90
CHEMBL4169247 1 7.80
CHEMBL4162555 1 7.80
CHEMBL4170833 1 7.80
CHEMBL4164738 1 7.70
CHEMBL4168237 1 7.70
CHEMBL4168775 1 7.60
CHEMBL4160139 1 7.40
CHEMBL4172568 1 7.40
CHEMBL4160463 1 7.40
CHEMBL4164247 1 7.30
CHEMBL4171579 1 7.20
CHEMBL4160965 1 7.20
CHEMBL2011441 1 7.20
CHEMBL4176082 1 7.10
CHEMBL4166246 1 7.00
CHEMBL4159115 1 6.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4172769 IC50 = 0.3162 nM 9.50
CHEMBL4167445 IC50 = 0.631 nM 9.20
CHEMBL4162364 IC50 = 1.0 nM 9.00
CHEMBL4172635 IC50 = 2.512 nM 8.60
CHEMBL4160218 IC50 = 2.512 nM 8.60
CHEMBL4175323 IC50 = 3.981 nM 8.40
CHEMBL4173046 IC50 = 3.981 nM 8.40
CHEMBL4160846 IC50 = 3.981 nM 8.40
CHEMBL4173861 IC50 = 7.943 nM 8.10
CHEMBL4165356 IC50 = 7.943 nM 8.10
CHEMBL4170431 IC50 = 10.0 nM 8.00
CHEMBL4162097 IC50 = 12.59 nM 7.90
CHEMBL4175972 IC50 = 12.59 nM 7.90
CHEMBL4165939 IC50 = 12.59 nM 7.90
CHEMBL4170833 IC50 = 15.85 nM 7.80
CHEMBL4162555 IC50 = 15.85 nM 7.80
CHEMBL4169247 IC50 = 15.85 nM 7.80
CHEMBL4164738 IC50 = 19.95 nM 7.70
CHEMBL4168237 IC50 = 19.95 nM 7.70
CHEMBL4168775 IC50 = 25.12 nM 7.60
CHEMBL4160139 IC50 = 39.81 nM 7.40
CHEMBL4172568 IC50 = 39.81 nM 7.40
CHEMBL4160463 IC50 = 39.81 nM 7.40
CHEMBL4164247 IC50 = 50.12 nM 7.30
CHEMBL2011441 IC50 = 63.1 nM 7.20
CHEMBL4160965 IC50 = 63.1 nM 7.20
CHEMBL4171579 IC50 = 63.1 nM 7.20
CHEMBL4176082 IC50 = 79.43 nM 7.10
CHEMBL4166246 IC50 = 100.0 nM 7.00
CHEMBL4159115 IC50 = 125.89 nM 6.90
CHEMBL4176859 IC50 = 125.89 nM 6.90
CHEMBL4176441 IC50 = 158.49 nM 6.80
CHEMBL4167390 IC50 = 158.49 nM 6.80
CHEMBL4165500 IC50 = 199.53 nM 6.70
CHEMBL4162503 IC50 = 199.53 nM 6.70
CHEMBL4174254 IC50 = 630.96 nM 6.20
CHEMBL4174488 IC50 = 630.96 nM 6.20
CHEMBL4175259 IC50 = 794.33 nM 6.10
CHEMBL4170786 IC50 = 1000.0 nM 6.00
CHEMBL4161268 IC50 = 1000.0 nM 6.00
CHEMBL4171873 IC50 = 1258.93 nM 5.90
CHEMBL4174872 IC50 = 3162.28 nM 5.50
CHEMBL4173424 IC50 = 3162.28 nM 5.50
CHEMBL4163571 IC50 = 3162.28 nM 5.50
CHEMBL4165828 IC50 = 5011.87 nM 5.30
CHEMBL4161922 IC50 = 5011.87 nM 5.30
CHEMBL4167021 IC50 = 5011.87 nM 5.30
CHEMBL4169258 IC50 = 7943.28 nM 5.10
CHEMBL4168920 IC50 = 10000.0 nM 5.00
CHEMBL4166980 IC50 > 10000.0 nM -