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Assay Detail

CHEMBL4630459

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

Binding
Antagonist activity at CCR4 in mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% mouse serum by CellTiter-Glo assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

C-C chemokine receptor type 4 (CHEMBL5410)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Novel Piperidinyl-Azetidines as Potent and Selective CCR4 Antagonists Elicit Antitumor Response as a Single Agent and in Combination with Checkpoint Inhibitors.
Robles O, Jackson JJ, Marshall L, Talay O, Chian D, Cutler G, Diokno R, Hu DX, Jacobson S, Karbarz E, Kassner PD, Ketcham JM, McKinnell J, Meleza C, Reilly MK, Riegler E, Shunatona HP, Wadsworth A, Younai A, Brockstedt DG, Wustrow DJ, Zibinsky M.
J Med Chem (2020) 63 : 8584 -8607
PubMed 32667798 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.41 7.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4637143 1 7.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4637143 IC50 = 39.0 nM 7.41