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Assay Detail

CHEMBL3102089

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

Binding
Displacement of [125I]MIP-1alpha from rat CCR1
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

C-C chemokine receptor type 1 (CHEMBL5499)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure activity relationships of fused bicyclic and urea derivatives of spirocyclic compounds as potent CCR1 antagonists.
Hossain N, Mensonides-Harsema M, Cooper ME, Eriksson T, Ivanova S, Bergström L.
Bioorg Med Chem Lett (2014) 24 : 108 -112
PubMed 24332486 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.46 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3099943 1 7.80
CHEMBL3099945 1 7.30
CHEMBL3099944 1 7.30
CHEMBL3099946 1 7.05
CHEMBL3099947 1 7.00
CHEMBL3099941 1 6.35
CHEMBL3099951 1 5.90
CHEMBL3099948 1 5.80
CHEMBL3099950 1 5.79
CHEMBL3099942 1 5.75
CHEMBL3099960 1 5.75
CHEMBL3099949 1 5.68
CHEMBL3099959 1 -
CHEMBL3099958 1 -
CHEMBL3099957 1 -
CHEMBL3099956 1 -
CHEMBL3099955 1 -
CHEMBL3099954 1 -
CHEMBL3099953 1 -
CHEMBL3099952 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3099943 IC50 = 16.0 nM 7.80
CHEMBL3099945 IC50 = 50.0 nM 7.30
CHEMBL3099944 IC50 = 50.0 nM 7.30
CHEMBL3099946 IC50 = 90.0 nM 7.05
CHEMBL3099947 IC50 = 101.0 nM 7.00
CHEMBL3099941 IC50 = 447.0 nM 6.35
CHEMBL3099951 IC50 = 1260.0 nM 5.90
CHEMBL3099948 IC50 = 1580.0 nM 5.80
CHEMBL3099950 IC50 = 1620.0 nM 5.79
CHEMBL3099942 IC50 = 1760.0 nM 5.75
CHEMBL3099960 IC50 = 1780.0 nM 5.75
CHEMBL3099949 IC50 = 2110.0 nM 5.68
CHEMBL3099959 IC50 - -
CHEMBL3099958 IC50 - -
CHEMBL3099957 IC50 - -
CHEMBL3099956 IC50 - -
CHEMBL3099955 IC50 - -
CHEMBL3099954 IC50 > 6000.0 nM -
CHEMBL3099953 IC50 - -
CHEMBL3099952 IC50 - -