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Assay Detail

CHEMBL867801

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

Binding
Displacement of [125I]I309 from human CCR8 expressed in L1.2 cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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
Ki 15 6.89 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL205993 1 8.22
CHEMBL380492 1 8.05
CHEMBL209350 1 7.96
CHEMBL204419 1 7.82
CHEMBL436753 1 7.64
CHEMBL381619 1 7.57
CHEMBL379834 1 7.22
CHEMBL205447 1 7.21
CHEMBL205457 1 6.60
CHEMBL210322 1 6.60
CHEMBL205692 1 5.85
CHEMBL205808 1 5.58
CHEMBL205304 1 5.04
CHEMBL381354 1 5.04
CHEMBL377931 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL205993 Ki = 6.0 nM 8.22
CHEMBL380492 Ki = 9.0 nM 8.05
CHEMBL209350 Ki = 11.0 nM 7.96
CHEMBL204419 Ki = 15.0 nM 7.82
CHEMBL436753 Ki = 23.0 nM 7.64
CHEMBL381619 Ki = 27.0 nM 7.57
CHEMBL379834 Ki = 60.0 nM 7.22
CHEMBL205447 Ki = 62.0 nM 7.21
CHEMBL205457 Ki = 250.0 nM 6.60
CHEMBL210322 Ki = 250.0 nM 6.60
CHEMBL205692 Ki = 1400.0 nM 5.85
CHEMBL205808 Ki = 2600.0 nM 5.58
CHEMBL205304 Ki = 9100.0 nM 5.04
CHEMBL381354 Ki = 9200.0 nM 5.04
CHEMBL377931 Ki > 30000.0 nM -