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Assay Detail

CHEMBL847899

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

Binding
Concentration required for inhibition of v-Abl receptor by tyrosine kinase enzyme assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Expert

Target

Tyrosine-protein kinase ABL (CHEMBL2111414)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

7-Pyrrolidinyl- and 7-piperidinyl-5-aryl-pyrrolo[2,3-d]pyrimidines--potent inhibitors of the tyrosine kinase c-Src.
Altmann E, Missbach M, Green J, Susa M, Wagenknecht HA, Widler L.
Bioorg Med Chem Lett (2001) 11 : 853 -856
PubMed 11277536 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.44 7.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL355019 1 7.27
CHEMBL262276 1 7.25
CHEMBL168921 1 7.24
CHEMBL169780 1 7.01
CHEMBL169920 1 6.92
CHEMBL408683 1 6.82
CHEMBL263528 1 6.68
CHEMBL171545 1 6.54
CHEMBL168661 1 6.44
CHEMBL274732 1 6.30
CHEMBL355269 1 6.29
CHEMBL169064 1 6.26
CHEMBL355891 1 6.23
CHEMBL355322 1 6.16
CHEMBL169065 1 6.00
CHEMBL169200 1 5.99
CHEMBL169519 1 5.85
CHEMBL168656 1 5.62
CHEMBL354033 1 5.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL355019 IC50 = 54.0 nM 7.27
CHEMBL262276 IC50 = 56.0 nM 7.25
CHEMBL168921 IC50 = 58.0 nM 7.24
CHEMBL169780 IC50 = 98.0 nM 7.01
CHEMBL169920 IC50 = 120.0 nM 6.92
CHEMBL408683 IC50 = 150.0 nM 6.82
CHEMBL263528 IC50 = 210.0 nM 6.68
CHEMBL171545 IC50 = 290.0 nM 6.54
CHEMBL168661 IC50 = 360.0 nM 6.44
CHEMBL274732 IC50 = 500.0 nM 6.30
CHEMBL355269 IC50 = 510.0 nM 6.29
CHEMBL169064 IC50 = 550.0 nM 6.26
CHEMBL355891 IC50 = 590.0 nM 6.23
CHEMBL355322 IC50 = 700.0 nM 6.16
CHEMBL169065 IC50 = 1000.0 nM 6.00
CHEMBL169200 IC50 = 1030.0 nM 5.99
CHEMBL169519 IC50 = 1400.0 nM 5.85
CHEMBL168656 IC50 = 2400.0 nM 5.62
CHEMBL354033 IC50 = 2800.0 nM 5.55