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Assay Detail

CHEMBL649936

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

Binding
Inhibitory concentration, binding towards C-C chemokine receptor type 5 using [125I]-MIP-1 alpha as radioligand expressed on CHO cells
ChEMBL ↗
61
Total Activities
61
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

1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 2: lead optimization affording selective, orally bioavailable compounds with potent anti-HIV activity.
Hale JJ, Budhu RJ, Holson EB, Finke PE, Oates B, Mills SG, MacCoss M, Gould SL, DeMartino JA, Springer MS, Siciliano S, Malkowitz L, Schleif WA, Hazuda D, Miller M, Kessler J, Danzeisen R, Holmes K, Lineberger J, Carella A, Carver G, Emini E.
Bioorg Med Chem Lett (2001) 11 : 2741 -2745
PubMed 11591514 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 61 7.57 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL93139 — — 1 10.00
CHEMBL328445 — — 1 10.00
CHEMBL431852 — — 1 9.70
CHEMBL329893 — — 1 9.70
CHEMBL327241 — — 1 9.10
CHEMBL328297 — — 1 9.10
CHEMBL328260 — — 1 9.10
CHEMBL93851 — — 1 8.70
CHEMBL430867 — — 1 8.70
CHEMBL329417 — — 1 8.40
CHEMBL329140 — — 1 8.40
CHEMBL92803 — — 1 8.30
CHEMBL85086 — — 1 8.15
CHEMBL327801 — — 1 8.05
CHEMBL93961 — — 1 7.92
CHEMBL327186 — — 1 7.82
CHEMBL96242 — — 1 7.77
CHEMBL94179 — — 1 7.72
CHEMBL315159 — — 1 7.72
CHEMBL92013 — — 1 7.66
CHEMBL406552 — — 1 7.66
CHEMBL330528 — — 1 7.58
CHEMBL430905 — — 1 7.51
CHEMBL327392 — — 1 7.50
CHEMBL329555 — — 1 7.48
CHEMBL92861 — — 1 7.47
CHEMBL327898 — — 1 7.34
CHEMBL94182 — — 1 7.34
CHEMBL93168 — — 1 7.32
CHEMBL93457 — — 1 7.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL93139 — IC50 = 0.1 nM 10.00
CHEMBL328445 — IC50 = 0.1 nM 10.00
CHEMBL329893 — IC50 = 0.2 nM 9.70
CHEMBL431852 — IC50 = 0.2 nM 9.70
CHEMBL327241 — IC50 = 0.8 nM 9.10
CHEMBL328297 — IC50 = 0.8 nM 9.10
CHEMBL328260 — IC50 = 0.8 nM 9.10
CHEMBL93851 — IC50 = 2.0 nM 8.70
CHEMBL430867 — IC50 = 2.0 nM 8.70
CHEMBL329417 — IC50 = 4.0 nM 8.40
CHEMBL329140 — IC50 = 4.0 nM 8.40
CHEMBL92803 — IC50 = 5.0 nM 8.30
CHEMBL85086 — IC50 = 7.0 nM 8.15
CHEMBL327801 — IC50 = 9.0 nM 8.05
CHEMBL93961 — IC50 = 12.0 nM 7.92
CHEMBL327186 — IC50 = 15.0 nM 7.82
CHEMBL96242 — IC50 = 17.0 nM 7.77
CHEMBL94179 — IC50 = 19.0 nM 7.72
CHEMBL315159 — IC50 = 19.0 nM 7.72
CHEMBL92013 — IC50 = 22.0 nM 7.66
CHEMBL406552 — IC50 = 22.0 nM 7.66
CHEMBL330528 — IC50 = 26.0 nM 7.58
CHEMBL430905 — IC50 = 31.0 nM 7.51
CHEMBL327392 — IC50 = 32.0 nM 7.50
CHEMBL329555 — IC50 = 33.0 nM 7.48
CHEMBL92861 — IC50 = 34.0 nM 7.47
CHEMBL94182 — IC50 = 46.0 nM 7.34
CHEMBL327898 — IC50 = 46.0 nM 7.34
CHEMBL93168 — IC50 = 48.0 nM 7.32
CHEMBL93457 — IC50 = 48.0 nM 7.32
CHEMBL329813 — IC50 = 52.0 nM 7.28
CHEMBL328373 — IC50 = 55.0 nM 7.26
CHEMBL329107 — IC50 = 57.0 nM 7.24
CHEMBL327846 — IC50 = 67.0 nM 7.17
CHEMBL92133 — IC50 = 89.0 nM 7.05
CHEMBL93949 — IC50 = 94.0 nM 7.03
CHEMBL90129 — IC50 = 96.0 nM 7.02
CHEMBL93625 — IC50 = 97.0 nM 7.01
CHEMBL327800 — IC50 = 140.0 nM 6.85
CHEMBL91793 — IC50 = 140.0 nM 6.85
CHEMBL96217 — IC50 = 150.0 nM 6.82
CHEMBL329131 — IC50 = 152.0 nM 6.82
CHEMBL93229 — IC50 = 155.0 nM 6.81
CHEMBL441635 — IC50 = 200.0 nM 6.70
CHEMBL330065 — IC50 = 220.0 nM 6.66
CHEMBL90015 — IC50 = 255.0 nM 6.59
CHEMBL327354 — IC50 = 260.0 nM 6.58
CHEMBL327540 — IC50 = 390.0 nM 6.41
CHEMBL91697 — IC50 = 480.0 nM 6.32
CHEMBL93644 — IC50 = 610.0 nM 6.21