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Compound Detail

CHEMBL1998112

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COc1ccc(-c2cc3nccn3c(Nc3ccccc3C(N)=O)n2)cc1OC

Basic Information

ChEMBL ID CHEMBL1998112
Phase Preclinical
Structure Type MOL
InChI Key CZQVOIDVDAVDFW-UHFFFAOYSA-N
24
Targets
24
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

389.4
MW (Da)
3.26
ALogP
7
HBA
2
HBD
103.8
PSA (Ų)
0.52
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 C21H19N5O3
MW 389.42
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.19

Activity Summary

Ki 24 meas. best 7.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase SYK
CHEMBL2599
Ki 7.9 7.9 12.6 1
Protein-tyrosine kinase 6
CHEMBL4601
Ki 7.5 7.5 31.6 1
Aurora kinase B
CHEMBL2185
Ki 7.5 7.5 31.6 1
Tyrosine-protein kinase Blk
CHEMBL2250
Ki 7.4 7.4 39.8 1
Aurora kinase A
CHEMBL4722
Ki 7.4 7.4 39.8 1
Proto-oncogene tyrosine-protein kinase ROS
CHEMBL5568
Ki 7.2 7.2 63.1 1
Tyrosine-protein kinase Lck
CHEMBL258
Ki 7.1 7.1 79.4 1
Vascular endothelial growth factor receptor 2
CHEMBL279
Ki 7.1 7.1 79.4 1
STE20-like serine/threonine-protein kinase
CHEMBL4202
Ki 7.0 7.0 100.0 1
Mitogen-activated protein kinase kinase kinase kinase 2
CHEMBL5330
Ki 6.9 6.9 125.9 1
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
Ki 6.8 6.8 158.5 1
Tyrosine-protein kinase BTK
CHEMBL5251
Ki 6.8 6.8 158.5 1
Proto-oncogene tyrosine-protein kinase receptor Ret
CHEMBL2041
Ki 6.7 6.7 199.5 1
Tyrosine-protein kinase Lyn
CHEMBL3905
Ki 6.7 6.7 199.5 1
Tyrosine-protein kinase Fer
CHEMBL3982
Ki 6.5 6.5 316.2 1
Insulin receptor
CHEMBL1981
Ki 6.3 6.3 501.2 1
Tyrosine-protein kinase JAK2
CHEMBL2971
Ki 6.1 6.1 794.3 1
Serine/threonine-protein kinase N2
CHEMBL3032
Ki 6.0 6.0 1000.0 1
Serine/threonine-protein kinase 17A
CHEMBL4525
Ki 5.9 5.9 1258.9 1
Receptor tyrosine-protein kinase erbB-4
CHEMBL3009
Ki 5.9 5.9 1258.9 1
Ribosomal protein S6 kinase alpha-3
CHEMBL2345
Ki 5.6 5.6 2511.9 1
Protein kinase C delta type
CHEMBL2996
Ki 5.4 5.4 3981.1 1
Mitogen-activated protein kinase kinase kinase kinase 4
CHEMBL6166
Ki 5.4 5.4 3981.1 1
SRSF protein kinase 1
CHEMBL4375
Ki 5.3 5.3 5011.9 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein kinase SYK Ki = 12.59 nM 7.9 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Aurora kinase B Ki = 31.62 nM 7.5 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Protein-tyrosine kinase 6 Ki = 31.62 nM 7.5 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Aurora kinase A Ki = 39.81 nM 7.4 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Tyrosine-protein kinase Blk Ki = 39.81 nM 7.4 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Proto-oncogene tyrosine-protein kinase ROS Ki = 63.1 nM 7.2 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Tyrosine-protein kinase Lck Ki = 79.43 nM 7.1 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Vascular endothelial growth factor receptor 2 Ki = 79.43 nM 7.1 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
STE20-like serine/threonine-protein kinase Ki = 100.0 nM 7.0 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Mitogen-activated protein kinase kinase kinase kinase 2 Ki = 125.89 nM 6.9 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Tyrosine-protein kinase BTK Ki = 158.49 nM 6.8 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Proto-oncogene tyrosine-protein kinase Src Ki = 158.49 nM 6.8 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Proto-oncogene tyrosine-protein kinase receptor Ret Ki = 199.53 nM 6.7 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Tyrosine-protein kinase Lyn Ki = 199.53 nM 6.7 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Tyrosine-protein kinase Fer Ki = 316.23 nM 6.5 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Insulin receptor Ki = 501.19 nM 6.3 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Tyrosine-protein kinase JAK2 Ki = 794.33 nM 6.1 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Serine/threonine-protein kinase N2 Ki = 1000.0 nM 6.0 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Serine/threonine-protein kinase 17A Ki = 1258.93 nM 5.9 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Receptor tyrosine-protein kinase erbB-4 Ki = 1258.93 nM 5.9 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -

Data from ChEMBL 36 via Core Engine