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Compound Detail

CHEMBL3647967

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C=CC(=O)N[C@H]1CC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)CC1

Basic Information

ChEMBL ID CHEMBL3647967
Phase Preclinical
Structure Type MOL
InChI Key SSDFTYWIYVWCIE-KDURUIRLSA-N
20
Targets
59
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

454.5
MW (Da)
4.65
ALogP
7
HBA
2
HBD
108.0
PSA (Ų)
0.41
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H26N6O2
MW 454.53
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -0.78

Activity Summary

IC50 59 meas. best 9.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase Blk
CHEMBL2250
IC50 9.7 9.7 0.2 2
Tyrosine-protein kinase Fgr
CHEMBL4454
IC50 9.4 9.4 0.4 2
Tyrosine-protein kinase BTK
CHEMBL5251
IC50 9.24 9.08 0.6 6
Tyrosine-protein kinase Yes
CHEMBL2073
IC50 9.1 9.1 0.8 2
Tyrosine-protein kinase Lck
CHEMBL258
IC50 9.0 9.0 1.0 8
Tyrosine-protein kinase HCK
CHEMBL3234
IC50 9.0 9.0 1.0 2
Cytoplasmic tyrosine-protein kinase BMX
CHEMBL3834
IC50 8.96 8.96 1.1 2
Tyrosine-protein kinase Lyn
CHEMBL3905
IC50 8.92 8.92 1.2 2
Tyrosine-protein kinase CSK
CHEMBL2634
IC50 8.62 8.62 2.4 2
Receptor tyrosine-protein kinase erbB-4
CHEMBL3009
IC50 8.49 7.5967 3.2 6
Protein-tyrosine kinase 6
CHEMBL4601
IC50 8.48 8.48 3.3 2
Tyrosine-protein kinase Fyn
CHEMBL1841
IC50 8.15 8.15 7.1 2
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
IC50 7.84 7.84 14.3 2
Epidermal growth factor receptor
CHEMBL203
IC50 7.69 7.69 20.6 4
Tyrosine-protein kinase ABL1
CHEMBL1862
IC50 7.49 7.49 32.3 2
Tyrosine-protein kinase Tec
CHEMBL4246
IC50 6.97 6.97 108.0 2
Tyrosine-protein kinase ITK/TSK
CHEMBL2959
IC50 6.04 6.04 909.9 4
Receptor tyrosine-protein kinase erbB-2
CHEMBL1824
IC50 5.81 5.81 1536.0 1
Tyrosine-protein kinase Fer
CHEMBL3982
IC50 5.47 5.47 3346.0 2
Tyrosine-protein kinase JAK3
CHEMBL2148
IC50 5.08 5.08 8278.0 4

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein kinase Blk IC50 = 0.2 nM 9.7 HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase as... -
Tyrosine-protein kinase Blk IC50 = 0.2 nM 9.7 In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot ... -
Tyrosine-protein kinase Fgr IC50 = 0.4 nM 9.4 In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot ... -
Tyrosine-protein kinase Fgr IC50 = 0.4 nM 9.4 HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase as... -
Tyrosine-protein kinase BTK IC50 = 0.58 nM 9.24 In Vitro Inhibition Assay: Measurements were performed in a reaction volume of 5... -
Tyrosine-protein kinase BTK IC50 = 0.58 nM 9.24 Time-Resolved Fluorescence Resonance Energy Transfer (TR-FRET) Assay: Btk kinase... -
Tyrosine-protein kinase Yes IC50 = 0.8 nM 9.1 HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase as... -
Tyrosine-protein kinase Yes IC50 = 0.8 nM 9.1 In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot ... -
Tyrosine-protein kinase Lck IC50 = 1.0 nM 9.0 HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase as... -
Tyrosine-protein kinase Lck IC50 = 1.0 nM 9.0 HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase as... -
Tyrosine-protein kinase BTK IC50 = 1.0 nM 9.0 HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase as... -
Tyrosine-protein kinase Lck IC50 = 1.0 nM 9.0 In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot ... -
Tyrosine-protein kinase HCK IC50 = 1.0 nM 9.0 HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase as... -
Tyrosine-protein kinase HCK IC50 = 1.0 nM 9.0 In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot ... -
Tyrosine-protein kinase Lck IC50 = 1.0 nM 9.0 In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot ... -
Tyrosine-protein kinase Lck IC50 = 1.0 nM 9.0 HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase as... -
Tyrosine-protein kinase Lck IC50 = 1.0 nM 9.0 HotSpot kinase assay: IC50s were determined using the in vitro HotSpot kinase as... -
Tyrosine-protein kinase Lck IC50 = 1.0 nM 9.0 In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot ... -
Tyrosine-protein kinase Lck IC50 = 1.0 nM 9.0 In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot ... -
Tyrosine-protein kinase BTK IC50 = 1.0 nM 9.0 In Vitro HotSpot Kinase Assay: IC50s were determined using the in vitro HotSpot ... -

Data from ChEMBL 36 via Core Engine