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Compound Detail

CHEMBL1970879

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COc1cc(-c2nn(C3CCC(N4CCN(C(C)=O)CC4)CC3)c3ncnc(N)c23)ccc1NC(=O)c1cc2ccccc2n1C

Basic Information

ChEMBL ID CHEMBL1970879
Phase Preclinical
Structure Type MOL
InChI Key ZMNWFTYYYCSSTF-UHFFFAOYSA-N
23
Targets
24
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

621.8
MW (Da)
4.48
ALogP
10
HBA
2
HBD
136.4
PSA (Ų)
0.28
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H39N9O3
MW 621.75
Aromatic Rings 5
Heavy Atoms 46
NP-Likeness -1.29

Activity Summary

Ki 22 meas. best 9.0
IC50 2 meas. best 6.83

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase Fyn
CHEMBL1841
Ki 9.0 9.0 1.0 1
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
Ki 8.5 8.5 3.2 1
Epidermal growth factor receptor
CHEMBL203
Ki 7.6 7.6 25.1 1
LIM domain kinase 1
CHEMBL3836
Ki 7.5 7.5 31.6 1
Receptor tyrosine-protein kinase erbB-2
CHEMBL1824
Ki 7.3 7.3 50.1 1
Receptor tyrosine-protein kinase erbB-4
CHEMBL3009
Ki 7.3 7.3 50.1 1
Tyrosine-protein kinase Lck
CHEMBL258
IC50 6.83 6.83 147.0 2
Tyrosine-protein kinase ABL1
CHEMBL1862
Ki 6.8 6.8 158.5 1
Serine/threonine-protein kinase MRCK alpha
CHEMBL4516
Ki 6.8 6.8 158.5 1
Aurora kinase B
CHEMBL2185
Ki 6.8 6.8 158.5 1
Aurora kinase A
CHEMBL4722
Ki 6.7 6.7 199.5 1
Serine/threonine-protein kinase Nek2
CHEMBL3835
Ki 6.7 6.7 199.5 1
Rho-associated protein kinase 1
CHEMBL3231
Ki 6.4 6.4 398.1 1
Serine/threonine-protein kinase PLK4
CHEMBL3788
Ki 6.4 6.4 398.1 1
Vascular endothelial growth factor receptor 1
CHEMBL1868
Ki 6.4 6.4 398.1 1
Serine/threonine-protein kinase PAK 4
CHEMBL4482
Ki 6.3 6.3 501.2 1
Serine/threonine-protein kinase Chk2
CHEMBL2527
Ki 6.1 6.1 794.3 1
Macrophage colony-stimulating factor 1 receptor
CHEMBL1844
Ki 6.1 6.1 794.3 1
Serine/threonine-protein kinase 3
CHEMBL4708
Ki 5.8 5.8 1584.9 1
High affinity nerve growth factor receptor
CHEMBL2815
Ki 5.7 5.7 1995.3 1
Serine/threonine-protein kinase PAK 1
CHEMBL4600
Ki 5.5 5.5 3162.3 1
Insulin receptor
CHEMBL1981
Ki 5.4 5.4 3981.1 1
Mitogen-activated protein kinase 1
CHEMBL4040
Ki 5.4 5.4 3981.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein kinase Fyn Ki = 1.0 nM 9.0 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Proto-oncogene tyrosine-protein kinase Src Ki = 3.162 nM 8.5 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Epidermal growth factor receptor Ki = 25.12 nM 7.6 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
LIM domain kinase 1 Ki = 31.62 nM 7.5 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Receptor tyrosine-protein kinase erbB-2 Ki = 50.12 nM 7.3 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Receptor tyrosine-protein kinase erbB-4 Ki = 50.12 nM 7.3 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Tyrosine-protein kinase Lck IC50 = 147.0 nM 6.83 Inhibition of LCK (unknown origin) 38316368
Tyrosine-protein kinase Lck IC50 = 147.0 nM 6.83 Inhibition of recombinant human LCK (64 to 509 residues) incubated for 60 mins i... 38316368
Serine/threonine-protein kinase MRCK alpha Ki = 158.49 nM 6.8 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Aurora kinase B Ki = 158.49 nM 6.8 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Tyrosine-protein kinase ABL1 Ki = 158.49 nM 6.8 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Serine/threonine-protein kinase Nek2 Ki = 199.53 nM 6.7 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... -
Serine/threonine-protein kinase PLK4 Ki = 398.11 nM 6.4 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Rho-associated protein kinase 1 Ki = 398.11 nM 6.4 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Vascular endothelial growth factor receptor 1 Ki = 398.11 nM 6.4 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Serine/threonine-protein kinase PAK 4 Ki = 501.19 nM 6.3 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Macrophage colony-stimulating factor 1 receptor Ki = 794.33 nM 6.1 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Serine/threonine-protein kinase Chk2 Ki = 794.33 nM 6.1 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Serine/threonine-protein kinase 3 Ki = 1584.89 nM 5.8 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -

Literature References

PubMed DOI Target Context # Activities
38316368 10.1016/j.bmcl.2024.129645 COLO 201 16
38316368 10.1016/j.bmcl.2024.129645 Tyrosine-protein kinase Lck 2

Data from ChEMBL 36 via Core Engine