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Assay Detail

CHEMBL3428282

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

ADMET
Cytotoxicity against human Jurkat T cells without TCR stimulation assessed as cell viability by ATPlite assay
14
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type Jurkat
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

ADMET (CHEMBL612558)
Type ADMET

Publication

Tetrahydroindazoles as Interleukin-2 Inducible T-Cell Kinase Inhibitors. Part II. Second-Generation Analogues with Enhanced Potency, Selectivity, and Pharmacodynamic Modulation in Vivo.
Burch JD, Barrett K, Chen Y, DeVoss J, Eigenbrot C, Goldsmith R, Ismaili MH, Lau K, Lin Z, Ortwine DF, Zarrin AA, McEwan PA, Barker JJ, Ellebrandt C, Kordt D, Stein DB, Wang X, Chen Y, Hu B, Xu X, Yuen PW, Zhang Y, Pei Z.
J Med Chem (2015) 58 : 3806 -3816
PubMed 25844760 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 4.61 5.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3298371 1 5.33
CHEMBL3426309 1 4.92
CHEMBL3426302 2 4.70
CHEMBL3426305 2 4.70
CHEMBL3426301 2 4.57
CHEMBL3426304 1 4.54
CHEMBL3426308 1 4.54
CHEMBL3426303 2 4.48
CHEMBL3426306 1 4.38
CHEMBL3298374 1 4.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3298371 IC50 = 4700.0 nM 5.33
CHEMBL3426309 IC50 = 12000.0 nM 4.92
CHEMBL3426305 IC50 = 20000.0 nM 4.70
CHEMBL3426302 IC50 = 20000.0 nM 4.70
CHEMBL3426301 IC50 = 27000.0 nM 4.57
CHEMBL3426304 IC50 = 29000.0 nM 4.54
CHEMBL3426308 IC50 = 29000.0 nM 4.54
CHEMBL3426305 IC50 = 30000.0 nM 4.52
CHEMBL3426303 IC50 = 33000.0 nM 4.48
CHEMBL3426306 IC50 = 42000.0 nM 4.38
CHEMBL3426302 IC50 = 44000.0 nM 4.36
CHEMBL3298374 IC50 = 57000.0 nM 4.24
CHEMBL3426301 IC50 > 50000.0 nM -
CHEMBL3426303 IC50 > 50000.0 nM -