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Assay Detail

CHEMBL812374

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

Functional
Immunosuppressive activity was determined as the ability to inhibit T cell proliferation.
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type T-cell
Confidence 1 — Organism
Curated By Expert

Target

T-cell (CHEMBL614309)
Type CELL-LINE

Publication

C32-O-imidazol-2-yl-methyl ether derivatives of the immunosuppressant ascomycin with improved therapeutic potential.
Goulet MT, McAlpine SR, Staruch MJ, Koprak S, Dumont FJ, Cryan JG, Wiederrecht GJ, Rosa R, Wilusz MB, Peterson LB, Wyvratt MJ, Parsons WH.
Bioorg Med Chem Lett (1998) 8 : 2253 -2258
PubMed 9873523 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 9.00 9.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL412818 1 9.74
CHEMBL266443 1 9.70
CHEMBL437410 1 9.49
CHEMBL440434 1 9.47
CHEMBL262995 1 9.44
CHEMBL442307 1 9.37
CHEMBL265122 1 9.35
CHEMBL262406 1 9.29
CHEMBL405517 1 9.24
CHEMBL8597 ASCOMYCIN 1 9.16
CHEMBL412201 1 9.15
CHEMBL428499 1 9.10
CHEMBL408603 1 9.07
CHEMBL437621 1 9.06
CHEMBL276133 1 8.96
CHEMBL428447 1 8.92
CHEMBL262667 1 8.72
CHEMBL385568 1 8.68
CHEMBL386482 1 8.59
CHEMBL306552 1 8.57
CHEMBL405682 1 8.39
CHEMBL263345 1 8.31
CHEMBL73289 1 8.13
CHEMBL268843 1 8.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL412818 IC50 = 0.18 nM 9.74
CHEMBL266443 IC50 = 0.2 nM 9.70
CHEMBL437410 IC50 = 0.32 nM 9.49
CHEMBL440434 IC50 = 0.34 nM 9.47
CHEMBL262995 IC50 = 0.36 nM 9.44
CHEMBL442307 IC50 = 0.43 nM 9.37
CHEMBL265122 IC50 = 0.45 nM 9.35
CHEMBL262406 IC50 = 0.51 nM 9.29
CHEMBL405517 IC50 = 0.58 nM 9.24
CHEMBL8597 ASCOMYCIN IC50 = 0.69 nM 9.16
CHEMBL412201 IC50 = 0.71 nM 9.15
CHEMBL428499 IC50 = 0.8 nM 9.10
CHEMBL408603 IC50 = 0.86 nM 9.07
CHEMBL437621 IC50 = 0.87 nM 9.06
CHEMBL276133 IC50 = 1.1 nM 8.96
CHEMBL428447 IC50 = 1.2 nM 8.92
CHEMBL262667 IC50 = 1.9 nM 8.72
CHEMBL385568 IC50 = 2.1 nM 8.68
CHEMBL386482 IC50 = 2.6 nM 8.59
CHEMBL306552 IC50 = 2.7 nM 8.57
CHEMBL405682 IC50 = 4.1 nM 8.39
CHEMBL263345 IC50 = 4.9 nM 8.31
CHEMBL73289 IC50 = 7.4 nM 8.13
CHEMBL268843 IC50 = 9.1 nM 8.04