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Assay Detail

CHEMBL701785

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

Functional
Immunosuppressive activity was measured by inhibition of the IL-2 production in Jurkat cells.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type Jurkat
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Peptidyl-prolyl cis-trans isomerase A (CHEMBL1949)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of non-immunosuppressive cyclophilin-Binding cyclosporin A derivatives as potential anti-HIV-1 drugs.
Evers M, Barrière JC, Bashiardes G, Bousseau A, Carry JC, Dereu N, Filoche B, Henin Y, Sablé S, Vuilhorgne M, Mignani S.
Bioorg Med Chem Lett (2003) 13 : 4415 -4419
PubMed 14643337 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.81 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL160 CYCLOSPORINE 4.0 1 8.70
CHEMBL3038087 1 8.52
CHEMBL2407581 1 7.82
CHEMBL3038089 1 7.72
CHEMBL3038081 1 7.33
CHEMBL3038084 1 7.21
CHEMBL3038088 1 7.01
CHEMBL2407585 1 6.96
CHEMBL3038093 1 6.89
CHEMBL3038092 1 6.78
CHEMBL442519 1 6.78
CHEMBL3038085 1 6.56
CHEMBL405301 1 6.11
CHEMBL3038082 1 6.05
CHEMBL3038091 1 6.03
CHEMBL3038086 1 6.02
CHEMBL1269597 SCY 635 2.0 1 5.81
CHEMBL3038083 1 5.80
CHEMBL3038090 1 5.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL160 CYCLOSPORINE IC50 = 2.0 nM 8.70
CHEMBL3038087 IC50 = 3.0 nM 8.52
CHEMBL2407581 IC50 = 15.0 nM 7.82
CHEMBL3038089 IC50 = 19.0 nM 7.72
CHEMBL3038081 IC50 = 47.0 nM 7.33
CHEMBL3038084 IC50 = 61.0 nM 7.21
CHEMBL3038088 IC50 = 97.0 nM 7.01
CHEMBL2407585 IC50 = 110.0 nM 6.96
CHEMBL3038093 IC50 = 128.0 nM 6.89
CHEMBL3038092 IC50 = 165.0 nM 6.78
CHEMBL442519 IC50 = 166.0 nM 6.78
CHEMBL3038085 IC50 = 277.0 nM 6.56
CHEMBL405301 IC50 = 783.0 nM 6.11
CHEMBL3038082 IC50 = 882.0 nM 6.05
CHEMBL3038091 IC50 = 934.0 nM 6.03
CHEMBL3038086 IC50 = 959.0 nM 6.02
CHEMBL1269597 SCY 635 IC50 = 1549.0 nM 5.81
CHEMBL3038083 IC50 = 1572.0 nM 5.80
CHEMBL3038090 IC50 = 6047.0 nM 5.22