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Assay Detail

CHEMBL702801

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

Binding
Inhibition of L-type Ca+2 channels
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Voltage-gated L-type calcium channel (CHEMBL2095229)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 4: synthesis of N-1 acidic functionality affording analogues with enhanced antiviral activity against HIV.
Lynch CL, Hale JJ, Budhu RJ, Gentry AL, Mills SG, Chapman KT, MacCoss M, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Cascieri MA, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Emini EA.
Bioorg Med Chem Lett (2002) 12 : 3001 -3004
PubMed 12270193 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.43 5.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20896 1 5.57
CHEMBL102826 1 5.28
CHEMBL319593 1 -
CHEMBL322693 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20896 IC50 = 2700.0 nM 5.57
CHEMBL102826 IC50 = 5300.0 nM 5.28
CHEMBL319593 IC50 > 10000.0 nM -
CHEMBL322693 IC50 > 10000.0 nM -