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Assay Detail

CHEMBL653180

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

Binding
Inhibitory activity against Calcineurin (CaN phosphatase)
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Protein phosphatase 3 catalytic subunit alpha (CHEMBL4445)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent immunosuppressive C32-O-arylethyl ether derivatives of ascomycin with reduced toxicity.
Armstrong HM, Wong F, Holmes MA, Sinclair PJ, Goulet MT, Dumont FJ, Staruch MJ, Koprak S, Peterson LB, Rosa R, Wilusz MB, Wiederrecht GJ, Cryan JG, Wyvratt MJ, Parsons WH.
Bioorg Med Chem Lett (1999) 9 : 2089 -2094
PubMed 10450987 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 8.20 8.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL407332 1 8.55
CHEMBL266705 1 8.40
CHEMBL268110 1 8.38
CHEMBL405917 1 8.31
CHEMBL412791 1 8.23
CHEMBL65863 1 8.14
CHEMBL264568 1 8.13
CHEMBL275103 1 8.10
CHEMBL305081 1 8.06
CHEMBL431368 1 8.06
CHEMBL269732 TACROLIMUS ANHYDROUS 4.0 1 7.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL407332 IC50 = 2.8 nM 8.55
CHEMBL266705 IC50 = 3.96 nM 8.40
CHEMBL268110 IC50 = 4.17 nM 8.38
CHEMBL405917 IC50 = 4.93 nM 8.31
CHEMBL412791 IC50 = 5.85 nM 8.23
CHEMBL65863 IC50 = 7.25 nM 8.14
CHEMBL264568 IC50 = 7.32 nM 8.13
CHEMBL275103 IC50 = 7.91 nM 8.10
CHEMBL305081 IC50 = 8.7 nM 8.06
CHEMBL431368 IC50 = 8.65 nM 8.06
CHEMBL269732 TACROLIMUS ANHYDROUS IC50 = 14.8 nM 7.83