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Assay Detail

CHEMBL893666

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

Binding
Binding Affinity at CCL3
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

C-C chemokine receptor type 1 (CHEMBL2413)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Piperazinyl CCR1 antagonists--optimization of human liver microsome stability.
Brown MF, Bahnck KB, Blumberg LC, Brissette WH, Burrell SA, Driscoll JP, Fedeles F, Fisher MB, Foti RS, Gladue RP, Guzman-Martinez A, Hayward MM, Lira PD, Lillie BM, Lu Y, Lundquist GD, McElroy EB, McGlynn MA, Paradis TJ, Poss CS, Roache JH, Shavnya A, Shepard RM, Trevena KA, Tylaska LA.
Bioorg Med Chem Lett (2007) 17 : 3109 -3112
PubMed 17383873 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.31 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL391238 1 8.10
CHEMBL234263 1 7.89
CHEMBL430166 1 7.64
CHEMBL391302 1 7.52
CHEMBL232656 BX 471 FREE BASE 2.0 1 7.51
CHEMBL234262 1 7.42
CHEMBL391239 1 7.36
CHEMBL391301 1 7.23
CHEMBL234606 1 6.32
CHEMBL234622 1 6.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL391238 IC50 = 8.0 nM 8.10
CHEMBL234263 IC50 = 13.0 nM 7.89
CHEMBL430166 IC50 = 23.0 nM 7.64
CHEMBL391302 IC50 = 30.0 nM 7.52
CHEMBL232656 BX 471 FREE BASE IC50 = 31.0 nM 7.51
CHEMBL234262 IC50 = 38.0 nM 7.42
CHEMBL391239 IC50 = 44.0 nM 7.36
CHEMBL391301 IC50 = 59.0 nM 7.23
CHEMBL234606 IC50 = 480.0 nM 6.32
CHEMBL234622 IC50 = 860.0 nM 6.07