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Assay Detail

CHEMBL3428283

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

Binding
Inhibition of LCK (unknown origin)
17
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tyrosine-protein kinase Lck (CHEMBL258)
Type SINGLE PROTEIN
Organism Homo sapiens

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
Ki 17 6.21 6.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3426301 2 6.68
CHEMBL3426302 2 6.62
CHEMBL3426308 1 6.58
CHEMBL3298371 1 6.47
CHEMBL3426309 1 6.34
CHEMBL3426304 1 6.22
CHEMBL3426307 1 6.22
CHEMBL3426303 2 6.19
CHEMBL3426305 2 6.18
CHEMBL3298369 1 5.85
CHEMBL3298374 1 5.75
CHEMBL3298288 1 5.75
CHEMBL3426306 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3426301 Ki = 210.0 nM 6.68
CHEMBL3426302 Ki = 240.0 nM 6.62
CHEMBL3426308 Ki = 260.0 nM 6.58
CHEMBL3426301 Ki = 260.0 nM 6.58
CHEMBL3298371 Ki = 340.0 nM 6.47
CHEMBL3426309 Ki = 460.0 nM 6.34
CHEMBL3426304 Ki = 600.0 nM 6.22
CHEMBL3426307 Ki = 600.0 nM 6.22
CHEMBL3426303 Ki = 640.0 nM 6.19
CHEMBL3426305 Ki = 660.0 nM 6.18
CHEMBL3426302 Ki = 1400.0 nM 5.85
CHEMBL3298369 Ki = 1400.0 nM 5.85
CHEMBL3426305 Ki = 1600.0 nM 5.80
CHEMBL3298288 Ki = 1800.0 nM 5.75
CHEMBL3298374 Ki = 1800.0 nM 5.75
CHEMBL3426303 Ki > 2500.0 nM -
CHEMBL3426306 Ki > 2500.0 nM -