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Assay Detail

CHEMBL855762

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

Binding
Binding affinity to human CCR8 expressed in L1.2 cells by FMAT assay
ChEMBL ↗
61
Total Activities
60
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 evaluation of naphthalene-sulfonamide antagonists of human CCR8.
Jenkins TJ, Guan B, Dai M, Li G, Lightburn TE, Huang S, Freeze BS, Burdi DF, Jacutin-Porte S, Bennett R, Chen W, Minor C, Ghosh S, Blackburn C, Gigstad KM, Jones M, Kolbeck R, Yin W, Smith S, Cardillo D, Ocain TD, Harriman GC.
J Med Chem (2007) 50 : 566 -584
PubMed 17266208 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 61 7.74 9.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL218374 — — 1 9.77
CHEMBL374939 — — 1 9.52
CHEMBL221865 — — 1 9.15
CHEMBL386308 — — 2 9.15
CHEMBL373739 — — 1 8.96
CHEMBL375854 — — 1 8.82
CHEMBL218375 — — 1 8.80
CHEMBL376910 — — 1 8.80
CHEMBL221867 — — 1 8.80
CHEMBL220701 — — 1 8.66
CHEMBL218037 — — 1 8.64
CHEMBL220753 — — 1 8.60
CHEMBL221130 — — 1 8.46
CHEMBL221904 — — 1 8.39
CHEMBL221251 — — 1 8.38
CHEMBL385108 — — 1 8.38
CHEMBL218503 — — 1 8.36
CHEMBL375315 — — 1 8.28
CHEMBL218036 — — 1 8.27
CHEMBL218218 — — 1 8.20
CHEMBL221977 — — 1 8.17
CHEMBL374979 — — 1 8.14
CHEMBL219433 — — 1 8.04
CHEMBL221021 — — 1 8.02
CHEMBL220703 — — 1 7.95
CHEMBL376076 — — 1 7.82
CHEMBL221961 — — 1 7.80
CHEMBL426207 — — 1 7.79
CHEMBL221345 — — 1 7.49
CHEMBL219327 — — 1 7.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL218374 — Ki = 0.17 nM 9.77
CHEMBL374939 — Ki = 0.3 nM 9.52
CHEMBL386308 — Ki = 0.7 nM 9.15
CHEMBL221865 — Ki = 0.7 nM 9.15
CHEMBL386308 — Ki = 1.0 nM 9.00
CHEMBL373739 — Ki = 1.1 nM 8.96
CHEMBL375854 — Ki = 1.5 nM 8.82
CHEMBL221867 — Ki = 1.6 nM 8.80
CHEMBL376910 — Ki = 1.6 nM 8.80
CHEMBL218375 — Ki = 1.6 nM 8.80
CHEMBL220701 — Ki = 2.2 nM 8.66
CHEMBL218037 — Ki = 2.3 nM 8.64
CHEMBL220753 — Ki = 2.5 nM 8.60
CHEMBL221130 — Ki = 3.5 nM 8.46
CHEMBL221904 — Ki = 4.1 nM 8.39
CHEMBL221251 — Ki = 4.2 nM 8.38
CHEMBL385108 — Ki = 4.2 nM 8.38
CHEMBL218503 — Ki = 4.4 nM 8.36
CHEMBL375315 — Ki = 5.21 nM 8.28
CHEMBL218036 — Ki = 5.4 nM 8.27
CHEMBL218218 — Ki = 6.3 nM 8.20
CHEMBL221977 — Ki = 6.7 nM 8.17
CHEMBL374979 — Ki = 7.2 nM 8.14
CHEMBL219433 — Ki = 9.1 nM 8.04
CHEMBL221021 — Ki = 9.5 nM 8.02
CHEMBL220703 — Ki = 11.3 nM 7.95
CHEMBL376076 — Ki = 15.2 nM 7.82
CHEMBL221961 — Ki = 15.8 nM 7.80
CHEMBL426207 — Ki = 16.4 nM 7.79
CHEMBL221345 — Ki = 32.1 nM 7.49
CHEMBL219327 — Ki = 34.3 nM 7.46
CHEMBL222058 — Ki = 35.7 nM 7.45
CHEMBL221789 — Ki = 37.9 nM 7.42
CHEMBL412116 — Ki = 42.6 nM 7.37
CHEMBL375880 — Ki = 45.6 nM 7.34
CHEMBL217979 — Ki = 50.9 nM 7.29
CHEMBL218366 — Ki = 71.0 nM 7.15
CHEMBL385288 — Ki = 77.4 nM 7.11
CHEMBL218350 — Ki = 77.7 nM 7.11
CHEMBL387451 — Ki = 81.1 nM 7.09
CHEMBL387161 — Ki = 108.0 nM 6.97
CHEMBL221078 — Ki = 114.0 nM 6.94
CHEMBL219589 — Ki = 125.6 nM 6.90
CHEMBL221638 — Ki = 199.0 nM 6.70
CHEMBL222111 — Ki = 233.1 nM 6.63
CHEMBL373504 — Ki = 243.0 nM 6.61
CHEMBL219487 — Ki = 566.5 nM 6.25
CHEMBL219588 — Ki = 578.0 nM 6.24
CHEMBL222110 — Ki = 1760.0 nM 5.75
CHEMBL386987 — Ki = 2033.0 nM 5.69