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Assay Detail

CHEMBL808764

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Binding
Inhibition of src kinase
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Proto-oncogene tyrosine-protein kinase Src (CHEMBL267)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

(S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta.
Jirousek MR, Gillig JR, Gonzalez CM, Heath WF, McDonald JH, Neel DA, Rito CJ, Singh U, Stramm LE, Melikian-Badalian A, Baevsky M, Ballas LM, Hall SE, Winneroski LL, Faul MM.
J Med Chem (1996) 39 : 2664 -2671
PubMed 8709095 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.00 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388978 STAUROSPORINE 1 9.00
CHEMBL419866 1 4.96
CHEMBL316239 1 4.05
CHEMBL311543 1 -
CHEMBL328229 1 -
CHEMBL315389 1 -
CHEMBL292495 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388978 STAUROSPORINE IC50 = 1.0 nM 9.00
CHEMBL419866 IC50 = 11000.0 nM 4.96
CHEMBL316239 IC50 = 89000.0 nM 4.05
CHEMBL311543 IC50 = - nM -
CHEMBL328229 IC50 > 100000.0 nM -
CHEMBL315389 IC50 > 100000.0 nM -
CHEMBL292495 IC50 > 100000.0 nM -