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Assay Detail

CHEMBL659084

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

Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
141
Total Activities
141
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 3: SAR studies on the benzylpyrazole segment.
Shu M, Loebach JL, Parker KA, Mills SG, Chapman KT, Shen DM, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Salvo JD, Lyons K, Pivnichny JV, Kwei GY, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller MD, Emini EA.
Bioorg Med Chem Lett (2004) 14 : 947 -952
PubMed 15012999 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 141 9.08 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL369235 1 9.70
CHEMBL366770 1 9.70
CHEMBL173400 1 9.70
CHEMBL174927 1 9.70
CHEMBL171958 1 9.70
CHEMBL427493 1 9.52
CHEMBL368329 1 9.52
CHEMBL174004 1 9.52
CHEMBL279992 1 9.52
CHEMBL172916 1 9.52
CHEMBL177127 1 9.52
CHEMBL435472 1 9.52
CHEMBL172894 1 9.52
CHEMBL367987 1 9.52
CHEMBL366868 1 9.52
CHEMBL369059 1 9.52
CHEMBL369812 1 9.40
CHEMBL366873 1 9.40
CHEMBL176669 1 9.40
CHEMBL175348 1 9.40
CHEMBL366611 1 9.40
CHEMBL176459 1 9.40
CHEMBL433793 1 9.40
CHEMBL174214 1 9.40
CHEMBL262402 1 9.40
CHEMBL177071 1 9.30
CHEMBL367416 1 9.30
CHEMBL367897 1 9.30
CHEMBL173583 1 9.30
CHEMBL368000 1 9.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL369235 IC50 = 0.2 nM 9.70
CHEMBL174927 IC50 = 0.2 nM 9.70
CHEMBL173400 IC50 = 0.2 nM 9.70
CHEMBL366770 IC50 = 0.2 nM 9.70
CHEMBL171958 IC50 = 0.2 nM 9.70
CHEMBL172916 IC50 = 0.3 nM 9.52
CHEMBL367987 IC50 = 0.3 nM 9.52
CHEMBL172894 IC50 = 0.3 nM 9.52
CHEMBL435472 IC50 = 0.3 nM 9.52
CHEMBL177127 IC50 = 0.3 nM 9.52
CHEMBL369059 IC50 = 0.3 nM 9.52
CHEMBL279992 IC50 = 0.3 nM 9.52
CHEMBL366868 IC50 = 0.3 nM 9.52
CHEMBL174004 IC50 = 0.3 nM 9.52
CHEMBL368329 IC50 = 0.3 nM 9.52
CHEMBL427493 IC50 = 0.3 nM 9.52
CHEMBL366873 IC50 = 0.4 nM 9.40
CHEMBL174214 IC50 = 0.4 nM 9.40
CHEMBL433793 IC50 = 0.4 nM 9.40
CHEMBL176459 IC50 = 0.4 nM 9.40
CHEMBL369812 IC50 = 0.4 nM 9.40
CHEMBL366611 IC50 = 0.4 nM 9.40
CHEMBL262402 IC50 = 0.4 nM 9.40
CHEMBL175348 IC50 = 0.4 nM 9.40
CHEMBL176669 IC50 = 0.4 nM 9.40
CHEMBL177071 IC50 = 0.5 nM 9.30
CHEMBL173583 IC50 = 0.5 nM 9.30
CHEMBL368000 IC50 = 0.5 nM 9.30
CHEMBL175079 IC50 = 0.5 nM 9.30
CHEMBL367416 IC50 = 0.5 nM 9.30
CHEMBL367897 IC50 = 0.5 nM 9.30
CHEMBL173479 IC50 = 0.5 nM 9.30
CHEMBL369478 IC50 = 0.5 nM 9.30
CHEMBL265723 IC50 = 0.5 nM 9.30
CHEMBL366610 IC50 = 0.5 nM 9.30
CHEMBL174996 IC50 = 0.5 nM 9.30
CHEMBL369398 IC50 = 0.5 nM 9.30
CHEMBL173091 IC50 = 0.5 nM 9.30
CHEMBL369593 IC50 = 0.5 nM 9.30
CHEMBL175341 IC50 = 0.5 nM 9.30
CHEMBL176528 IC50 = 0.5 nM 9.30
CHEMBL173254 IC50 = 0.6 nM 9.22
CHEMBL369659 IC50 = 0.6 nM 9.22
CHEMBL369494 IC50 = 0.6 nM 9.22
CHEMBL367560 IC50 = 0.6 nM 9.22
CHEMBL408800 IC50 = 0.6 nM 9.22
CHEMBL172296 IC50 = 0.6 nM 9.22
CHEMBL176426 IC50 = 0.6 nM 9.22
CHEMBL368467 IC50 = 0.6 nM 9.22
CHEMBL176933 IC50 = 0.6 nM 9.22