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Compound Detail

CHEMBL1994724

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COc1cccc(C(C)NC(=O)c2ccc(-c3ccncc3)s2)c1

Basic Information

ChEMBL ID CHEMBL1994724
Phase Preclinical
Structure Type MOL
InChI Key SJLQDZDKTVBBLP-UHFFFAOYSA-N
16
Targets
16
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

338.4
MW (Da)
4.31
ALogP
4
HBA
1
HBD
51.2
PSA (Ų)
0.75
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H18N2O2S
MW 338.43
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -1.34

Activity Summary

Ki 16 meas. best 8.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Rho-associated protein kinase 1
CHEMBL3231
Ki 8.9 8.9 1.3 1
cAMP-dependent protein kinase catalytic subunit alpha
CHEMBL4101
Ki 7.1 7.1 79.4 1
Serine/threonine-protein kinase Chk1
CHEMBL4630
Ki 7.1 7.1 79.4 1
Aurora kinase A
CHEMBL4722
Ki 6.7 6.7 199.5 1
Protein kinase C theta type
CHEMBL3920
Ki 6.5 6.5 316.2 1
Dual specificity protein kinase CLK4
CHEMBL4203
Ki 6.5 6.5 316.2 1
Aurora kinase B
CHEMBL2185
Ki 6.4 6.4 398.1 1
Glycogen synthase kinase-3 alpha
CHEMBL2850
Ki 6.0 6.0 1000.0 1
G protein-coupled receptor kinase 5
CHEMBL5678
Ki 6.0 6.0 1000.0 1
Glycogen synthase kinase-3 beta
CHEMBL262
Ki 5.9 5.9 1258.9 1
Ribosomal protein S6 kinase alpha-3
CHEMBL2345
Ki 5.8 5.8 1584.9 1
Casein kinase I isoform alpha
CHEMBL2793
Ki 5.8 5.8 1584.9 1
cAMP-dependent protein kinase catalytic subunit PRKX
CHEMBL5818
Ki 5.7 5.7 1995.3 1
Activin receptor type-1
CHEMBL5903
Ki 5.6 5.6 2511.9 1
Cyclin-dependent kinase 8
CHEMBL5719
Ki 5.5 5.5 3162.3 1
Mitogen-activated protein kinase kinase kinase kinase 4
CHEMBL6166
Ki 5.3 5.3 5011.9 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Rho-associated protein kinase 1 Ki = 1.259 nM 8.9 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Serine/threonine-protein kinase Chk1 Ki = 79.43 nM 7.1 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
cAMP-dependent protein kinase catalytic subunit alpha Ki = 79.43 nM 7.1 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Aurora kinase A Ki = 199.53 nM 6.7 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Protein kinase C theta type Ki = 316.23 nM 6.5 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Dual specificity protein kinase CLK4 Ki = 316.23 nM 6.5 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Aurora kinase B Ki = 398.11 nM 6.4 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
G protein-coupled receptor kinase 5 Ki = 1000.0 nM 6.0 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Glycogen synthase kinase-3 alpha Ki = 1000.0 nM 6.0 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Glycogen synthase kinase-3 beta Ki = 1258.93 nM 5.9 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Ribosomal protein S6 kinase alpha-3 Ki = 1584.89 nM 5.8 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Casein kinase I isoform alpha Ki = 1584.89 nM 5.8 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
cAMP-dependent protein kinase catalytic subunit PRKX Ki = 1995.26 nM 5.7 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Activin receptor type-1 Ki = 2511.89 nM 5.6 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Cyclin-dependent kinase 8 Ki = 3162.28 nM 5.5 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Mitogen-activated protein kinase kinase kinase kinase 4 Ki = 5011.87 nM 5.3 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -

Data from ChEMBL 36 via Core Engine