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Assay Detail

CHEMBL3579780

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

Binding
Inhibition of [125I]MCP1-beta binding to CCR5 in human HT1080 cell membranes incubated for 4 to 6 hrs
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HT-1080
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

C-C chemokine receptor type 5 (CHEMBL274)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a Potent and Orally Bioavailable Dual Antagonist of CC Chemokine Receptors 2 and 5.
Carter PH, Brown GD, Cherney RJ, Batt DG, Chen J, Clark CM, Cvijic ME, Duncia JV, Ko SS, Mandlekar S, Mo R, Nelson DJ, Pang J, Rose AV, Santella JB, Tebben AJ, Traeger SC, Xu S, Zhao Q, Barrish JC.
ACS Med Chem Lett (2015) 6 : 439 -444
PubMed 25893046 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.59 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3577945 1 8.62
CHEMBL3577946 1 8.52
CHEMBL3577942 1 8.47
CHEMBL3577948 1 8.00
CHEMBL3577949 1 7.75
CHEMBL3577944 1 7.66
CHEMBL3577932 1 6.86
CHEMBL3577933 1 6.49
CHEMBL3577934 1 5.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3577945 IC50 = 2.4 nM 8.62
CHEMBL3577946 IC50 = 3.0 nM 8.52
CHEMBL3577942 IC50 = 3.4 nM 8.47
CHEMBL3577948 IC50 = 10.0 nM 8.00
CHEMBL3577949 IC50 = 18.0 nM 7.75
CHEMBL3577944 IC50 = 22.0 nM 7.66
CHEMBL3577932 IC50 = 137.0 nM 6.86
CHEMBL3577933 IC50 = 321.0 nM 6.49
CHEMBL3577934 IC50 = 1242.0 nM 5.91