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Compound Detail

CHEMBL1996780

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CCOC(=O)c1cn(-c2ccc(O)cc2C)c2cc(-c3ccncc3)ccc2c1=O

Basic Information

ChEMBL ID CHEMBL1996780
Phase Preclinical
Structure Type MOL
InChI Key WNMXOXGXHRHBLO-UHFFFAOYSA-N
11
Targets
11
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

400.4
MW (Da)
4.24
ALogP
6
HBA
1
HBD
81.4
PSA (Ų)
0.52
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H20N2O4
MW 400.43
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -0.50

Activity Summary

Ki 11 meas. best 7.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Rho-associated protein kinase 2
CHEMBL2973
Ki 7.5 7.5 31.6 1
Rho-associated protein kinase 1
CHEMBL3231
Ki 6.8 6.8 158.5 1
Serine/threonine-protein kinase MRCK alpha
CHEMBL4516
Ki 6.6 6.6 251.2 1
Protein kinase C delta type
CHEMBL2996
Ki 6.3 6.3 501.2 1
cAMP-dependent protein kinase catalytic subunit alpha
CHEMBL4101
Ki 5.9 5.9 1258.9 1
Cyclin-dependent kinase 2
CHEMBL301
Ki 5.4 5.4 3981.1 1
Cyclin-dependent kinase 1
CHEMBL308
Ki 5.4 5.4 3981.1 1
Cyclin-dependent kinase 5
CHEMBL4036
Ki 5.3 5.3 5011.9 1
Casein kinase I isoform delta
CHEMBL2828
Ki 5.2 5.2 6309.6 1
Serine/threonine-protein kinase MARK2
CHEMBL3831
Ki 5.2 5.2 6309.6 1
Glycogen synthase kinase-3 alpha
CHEMBL2850
Ki 5.1 5.1 7943.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Rho-associated protein kinase 2 Ki = 31.62 nM 7.5 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Rho-associated protein kinase 1 Ki = 158.49 nM 6.8 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Serine/threonine-protein kinase MRCK alpha Ki = 251.19 nM 6.6 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Protein kinase C delta type Ki = 501.19 nM 6.3 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
cAMP-dependent protein kinase catalytic subunit alpha Ki = 1258.93 nM 5.9 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Cyclin-dependent kinase 2 Ki = 3981.07 nM 5.4 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Cyclin-dependent kinase 1 Ki = 3981.07 nM 5.4 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Cyclin-dependent kinase 5 Ki = 5011.87 nM 5.3 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Casein kinase I isoform delta Ki = 6309.57 nM 5.2 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Serine/threonine-protein kinase MARK2 Ki = 6309.57 nM 5.2 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Glycogen synthase kinase-3 alpha Ki = 7943.28 nM 5.1 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -

Data from ChEMBL 36 via Core Engine