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Assay Detail

CHEMBL951105

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

Functional
Inhibition of anti-CD3-induced IL2 production in human whole blood by ELISA
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Tissue Blood
Confidence 1 — Organism
Curated By Autocuration

Target

Blood (CHEMBL613416)
Type TISSUE
Organism Homo sapiens

Publication

Structure-guided design of aminopyrimidine amides as potent, selective inhibitors of lymphocyte specific kinase: synthesis, structure-activity relationships, and inhibition of in vivo T cell activation.
DiMauro EF, Newcomb J, Nunes JJ, Bemis JE, Boucher C, Chai L, Chaffee SC, Deak HL, Epstein LF, Faust T, Gallant P, Gore A, Gu Y, Henkle B, Hsieh F, Huang X, Kim JL, Lee JH, Martin MW, McGowan DC, Metz D, Mohn D, Morgenstern KA, Oliveira-dos-Santos A, Patel VF, Powers D, Rose PE, Schneider S, Tomlinson SA, Tudor YY, Turci SM, Welcher AA, Zhao H, Zhu L, Zhu X.
J Med Chem (2008) 51 : 1681 -1694
PubMed 18321037 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.64 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL271140 1 8.70
CHEMBL272888 1 8.15
CHEMBL271141 1 7.89
CHEMBL407063 1 7.80
CHEMBL272850 1 7.37
CHEMBL411632 1 5.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL271140 IC50 = 2.0 nM 8.70
CHEMBL272888 IC50 = 7.0 nM 8.15
CHEMBL271141 IC50 = 13.0 nM 7.89
CHEMBL407063 IC50 = 16.0 nM 7.80
CHEMBL272850 IC50 = 43.0 nM 7.37
CHEMBL411632 IC50 = 1270.0 nM 5.90