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Assay Detail

CHEMBL3374865

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

Binding
Displacement of [125J]-eotaxin-1 from human CCR3 transfected in human K562 cells
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type K562
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

C-C chemokine receptor type 3 (CHEMBL3473)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Rodent selectivity of piperidine-4-yl-1H-indoles, a series of CC chemokine receptor-3 (CCR3) antagonists: insights from a receptor model.
Kriegl JM, Martyres D, Grundl MA, Anderskewitz R, Dollinger H, Rast G, Schmid B, Seither P, Tautermann CS.
Bioorg Med Chem Lett (2015) 25 : 229 -235
PubMed 25497216 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 35 7.31 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3355965 1 8.40
CHEMBL3355940 1 8.37
CHEMBL3355954 1 8.33
CHEMBL3355944 1 8.32
CHEMBL3355953 1 8.31
CHEMBL3355962 1 8.30
CHEMBL3355960 1 8.30
CHEMBL3355932 1 8.24
CHEMBL3355964 1 7.96
CHEMBL3355956 1 7.80
CHEMBL3355942 1 7.51
CHEMBL3355934 1 7.50
CHEMBL3355938 1 7.48
CHEMBL3355966 1 7.47
CHEMBL3355950 1 7.42
CHEMBL3355945 1 7.34
CHEMBL3355959 1 7.27
CHEMBL3355933 1 7.22
CHEMBL3355961 1 7.22
CHEMBL3355952 1 7.21
CHEMBL3355943 1 7.18
CHEMBL3355951 1 7.17
CHEMBL3355935 1 7.11
CHEMBL3355957 1 7.09
CHEMBL3355946 1 7.07
CHEMBL3355936 1 7.02
CHEMBL3355963 1 7.01
CHEMBL3355939 1 7.00
CHEMBL3355958 1 6.92
CHEMBL3355947 1 6.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3355965 Ki = 4.0 nM 8.40
CHEMBL3355940 Ki = 4.3 nM 8.37
CHEMBL3355954 Ki = 4.7 nM 8.33
CHEMBL3355944 Ki = 4.8 nM 8.32
CHEMBL3355953 Ki = 4.9 nM 8.31
CHEMBL3355962 Ki = 5.0 nM 8.30
CHEMBL3355960 Ki = 5.0 nM 8.30
CHEMBL3355932 Ki = 5.7 nM 8.24
CHEMBL3355964 Ki = 11.0 nM 7.96
CHEMBL3355956 Ki = 16.0 nM 7.80
CHEMBL3355942 Ki = 31.0 nM 7.51
CHEMBL3355934 Ki = 32.0 nM 7.50
CHEMBL3355938 Ki = 33.0 nM 7.48
CHEMBL3355966 Ki = 34.0 nM 7.47
CHEMBL3355950 Ki = 38.0 nM 7.42
CHEMBL3355945 Ki = 46.0 nM 7.34
CHEMBL3355959 Ki = 54.0 nM 7.27
CHEMBL3355933 Ki = 60.0 nM 7.22
CHEMBL3355961 Ki = 60.0 nM 7.22
CHEMBL3355952 Ki = 61.0 nM 7.21
CHEMBL3355943 Ki = 66.0 nM 7.18
CHEMBL3355951 Ki = 67.0 nM 7.17
CHEMBL3355935 Ki = 78.0 nM 7.11
CHEMBL3355957 Ki = 82.0 nM 7.09
CHEMBL3355946 Ki = 86.0 nM 7.07
CHEMBL3355936 Ki = 96.0 nM 7.02
CHEMBL3355963 Ki = 98.0 nM 7.01
CHEMBL3355939 Ki = 99.0 nM 7.00
CHEMBL3355958 Ki = 120.0 nM 6.92
CHEMBL3355947 Ki = 190.0 nM 6.72
CHEMBL3355948 Ki = 310.0 nM 6.51
CHEMBL3355937 Ki = 450.0 nM 6.35
CHEMBL3355941 Ki = 480.0 nM 6.32
CHEMBL3355949 Ki = 4000.0 nM 5.40
CHEMBL3355955 Ki = 6900.0 nM 5.16