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Assay Detail

CHEMBL769387

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Binding
Ability to inhibit autophosphorylation of immunopurified p56Ick
19
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Bicyclic compounds as ring-constrained inhibitors of protein-tyrosine kinase p56lck.
Burke TR, Lim B, Marquez VE, Li ZH, Bolen JB, Stefanova I, Horak ID.
J Med Chem (1993) 36 : 425 -432
PubMed 8474097 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 4.94 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL413118 1 6.70
CHEMBL48384 1 6.30
CHEMBL296407 2 4.66
CHEMBL18276 1 4.60
CHEMBL341423 1 4.58
CHEMBL139269 1 4.00
CHEMBL450329 1 4.00
CHEMBL336450 1 -
CHEMBL137114 1 -
CHEMBL137813 2 -
CHEMBL136636 1 -
CHEMBL308048 1 -
CHEMBL133937 1 -
CHEMBL295939 1 -
CHEMBL136344 1 -
CHEMBL136954 1 -
CHEMBL132379 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL413118 IC50 = 200.0 nM 6.70
CHEMBL48384 IC50 = 500.0 nM 6.30
CHEMBL296407 IC50 = 22000.0 nM 4.66
CHEMBL296407 IC50 = 22000.0 nM 4.66
CHEMBL18276 IC50 = 25000.0 nM 4.60
CHEMBL341423 IC50 = 26000.0 nM 4.58
CHEMBL139269 IC50 = 100000.0 nM 4.00
CHEMBL450329 IC50 = 100000.0 nM 4.00
CHEMBL336450 IC50 = 500000.0 nM -
CHEMBL137114 IC50 > 2000000.0 nM -
CHEMBL137813 IC50 = 1500000.0 nM -
CHEMBL136636 IC50 = 610000.0 nM -
CHEMBL137813 IC50 = 1500000.0 nM -
CHEMBL308048 IC50 = 1000000.0 nM -
CHEMBL133937 IC50 = 750000.0 nM -
CHEMBL295939 IC50 = 1900000.0 nM -
CHEMBL136344 IC50 = 2000000.0 nM -
CHEMBL136954 IC50 = 1500000.0 nM -
CHEMBL132379 IC50 > 2000000.0 nM -