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Assay Detail

CHEMBL822437

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

Binding
Inhibition of p60 c-Src tyrosine kinase enzyme activity in liquid-phase tyrosine phosphorylation assay at 830 ng/mL
41
Total Activities
41
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

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 41 7.32 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL263528 1 9.00
CHEMBL169780 1 9.00
CHEMBL169920 1 8.52
CHEMBL355019 1 8.52
CHEMBL408683 1 8.40
CHEMBL169939 1 8.30
CHEMBL168921 1 8.30
CHEMBL171545 1 8.22
CHEMBL168661 1 8.22
CHEMBL422565 1 8.10
CHEMBL352829 1 7.82
CHEMBL172514 1 7.82
CHEMBL169064 1 7.66
CHEMBL169043 1 7.62
CHEMBL169200 1 7.57
CHEMBL352666 1 7.46
CHEMBL354033 1 7.43
CHEMBL355322 1 7.42
CHEMBL274732 1 7.33
CHEMBL355891 1 7.30
CHEMBL168462 1 7.30
CHEMBL169519 1 7.28
CHEMBL355269 1 7.17
CHEMBL169065 1 7.08
CHEMBL172574 1 7.02
CHEMBL170726 1 7.00
CHEMBL353630 1 6.89
CHEMBL168560 1 6.89
CHEMBL353823 1 6.75
CHEMBL168829 1 6.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL263528 IC50 = 1.0 nM 9.00
CHEMBL169780 IC50 = 1.0 nM 9.00
CHEMBL355019 IC50 = 3.0 nM 8.52
CHEMBL169920 IC50 = 3.0 nM 8.52
CHEMBL408683 IC50 = 4.0 nM 8.40
CHEMBL169939 IC50 = 5.0 nM 8.30
CHEMBL168921 IC50 = 5.0 nM 8.30
CHEMBL171545 IC50 = 6.0 nM 8.22
CHEMBL168661 IC50 = 6.0 nM 8.22
CHEMBL422565 IC50 = 8.0 nM 8.10
CHEMBL172514 IC50 = 15.0 nM 7.82
CHEMBL352829 IC50 = 15.0 nM 7.82
CHEMBL169064 IC50 = 22.0 nM 7.66
CHEMBL169043 IC50 = 24.0 nM 7.62
CHEMBL169200 IC50 = 27.0 nM 7.57
CHEMBL352666 IC50 = 35.0 nM 7.46
CHEMBL354033 IC50 = 37.0 nM 7.43
CHEMBL355322 IC50 = 38.0 nM 7.42
CHEMBL274732 IC50 = 47.0 nM 7.33
CHEMBL168462 IC50 = 50.0 nM 7.30
CHEMBL355891 IC50 = 50.0 nM 7.30
CHEMBL169519 IC50 = 53.0 nM 7.28
CHEMBL355269 IC50 = 67.0 nM 7.17
CHEMBL169065 IC50 = 84.0 nM 7.08
CHEMBL172574 IC50 = 95.0 nM 7.02
CHEMBL170726 IC50 = 100.0 nM 7.00
CHEMBL353630 IC50 = 130.0 nM 6.89
CHEMBL168560 IC50 = 130.0 nM 6.89
CHEMBL353823 IC50 = 180.0 nM 6.75
CHEMBL168829 IC50 = 230.0 nM 6.64
CHEMBL168656 IC50 = 270.0 nM 6.57
CHEMBL367933 IC50 = 300.0 nM 6.52
CHEMBL353456 IC50 = 300.0 nM 6.52
CHEMBL352652 IC50 = 300.0 nM 6.52
CHEMBL434105 IC50 = 350.0 nM 6.46
CHEMBL352619 IC50 = 400.0 nM 6.40
CHEMBL169202 IC50 = 410.0 nM 6.39
CHEMBL352510 IC50 = 600.0 nM 6.22
CHEMBL167537 IC50 = 2000.0 nM 5.70
CHEMBL170004 IC50 = 5000.0 nM 5.30
CHEMBL262276 IC50 < 1.0 nM -