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Assay Detail

CHEMBL867802

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

Functional
Inhibition of I309-induced chemotaxis in L1.2 cells expressing CCR8
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type L1.2
Confidence 9 — Direct single protein target
Curated By Expert

Target

C-C chemokine receptor type 8 (CHEMBL4596)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and progress toward optimization of potent small molecule antagonists of CC chemokine receptor 8 (CCR8).
Ghosh S, Elder A, Guo J, Mani U, Patane M, Carson K, Ye Q, Bennett R, Chi S, Jenkins T, Guan B, Kolbeck R, Smith S, Zhang C, LaRosa G, Jaffee B, Yang H, Eddy P, Lu C, Uttamsingh V, Horlick R, Harriman G, Flynn D.
J Med Chem (2006) 49 : 2669 -2672
PubMed 16640325 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.84 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL205993 1 9.00
CHEMBL380492 1 8.40
CHEMBL205447 1 7.96
CHEMBL381619 1 7.66
CHEMBL204419 1 7.37
CHEMBL210322 1 7.26
CHEMBL209350 1 7.25
CHEMBL205808 1 -
CHEMBL205457 1 -
CHEMBL205692 1 -
CHEMBL381354 1 -
CHEMBL205304 1 -
CHEMBL377931 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL205993 IC50 = 1.0 nM 9.00
CHEMBL380492 IC50 = 4.0 nM 8.40
CHEMBL205447 IC50 = 11.0 nM 7.96
CHEMBL381619 IC50 = 22.0 nM 7.66
CHEMBL204419 IC50 = 43.0 nM 7.37
CHEMBL210322 IC50 = 55.0 nM 7.26
CHEMBL209350 IC50 = 56.0 nM 7.25
CHEMBL205808 IC50 - -
CHEMBL205457 IC50 - -
CHEMBL205692 IC50 - -
CHEMBL381354 IC50 - -
CHEMBL205304 IC50 - -
CHEMBL377931 IC50 - -