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Compound Detail

CHEMBL1973961

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COc1cc(N2CCN(C)CC2)ccc1C(=O)Nc1n[nH]c2ccc(Cc3cc(F)cc(F)c3)cc12

Basic Information

ChEMBL ID CHEMBL1973961
Phase Preclinical
Structure Type MOL
InChI Key DSSRVQAIWBZWON-UHFFFAOYSA-N
17
Targets
17
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

491.5
MW (Da)
4.44
ALogP
5
HBA
2
HBD
73.5
PSA (Ų)
0.42
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 C27H27F2N5O2
MW 491.54
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -1.41

Activity Summary

Ki 17 meas. best 7.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Leukocyte tyrosine kinase receptor
CHEMBL5627
Ki 7.9 7.9 12.6 1
ALK tyrosine kinase receptor
CHEMBL4247
Ki 7.4 7.4 39.8 1
Wee1-like protein kinase
CHEMBL5491
Ki 7.1 7.1 79.4 1
Proto-oncogene tyrosine-protein kinase ROS
CHEMBL5568
Ki 6.9 6.9 125.9 1
Serine/threonine-protein kinase PLK4
CHEMBL3788
Ki 6.6 6.6 251.2 1
NT-3 growth factor receptor
CHEMBL5608
Ki 6.3 6.3 501.2 1
Focal adhesion kinase 1
CHEMBL2695
Ki 6.2 6.2 631.0 1
High affinity nerve growth factor receptor
CHEMBL2815
Ki 6.2 6.2 631.0 1
Tyrosine-protein kinase Fer
CHEMBL3982
Ki 6.0 6.0 1000.0 1
Tyrosine-protein kinase FRK
CHEMBL4223
Ki 5.9 5.9 1258.9 1
Macrophage-stimulating protein receptor
CHEMBL2689
Ki 5.9 5.9 1258.9 1
Mitogen-activated protein kinase kinase kinase kinase 5
CHEMBL4852
Ki 5.7 5.7 1995.3 1
Activated CDC42 kinase 1
CHEMBL4599
Ki 5.6 5.6 2511.9 1
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
CHEMBL5543
Ki 5.6 5.6 2511.9 1
Mitogen-activated protein kinase 8
CHEMBL2276
Ki 5.5 5.5 3162.3 1
Protein kinase C gamma type
CHEMBL2938
Ki 5.4 5.4 3981.1 1
Death-associated protein kinase 3
CHEMBL2468
Ki 5.4 5.4 3981.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Leukocyte tyrosine kinase receptor Ki = 12.59 nM 7.9 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
ALK tyrosine kinase receptor Ki = 39.81 nM 7.4 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Wee1-like protein kinase Ki = 79.43 nM 7.1 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Proto-oncogene tyrosine-protein kinase ROS Ki = 125.89 nM 6.9 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Serine/threonine-protein kinase PLK4 Ki = 251.19 nM 6.6 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
NT-3 growth factor receptor Ki = 501.19 nM 6.3 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
High affinity nerve growth factor receptor Ki = 630.96 nM 6.2 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Focal adhesion kinase 1 Ki = 630.96 nM 6.2 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Tyrosine-protein kinase Fer Ki = 1000.0 nM 6.0 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Macrophage-stimulating protein receptor Ki = 1258.93 nM 5.9 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Tyrosine-protein kinase FRK Ki = 1258.93 nM 5.9 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Mitogen-activated protein kinase kinase kinase kinase 5 Ki = 1995.26 nM 5.7 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Dual specificity tyrosine-phosphorylation-regulated kinase 1B Ki = 2511.89 nM 5.6 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Activated CDC42 kinase 1 Ki = 2511.89 nM 5.6 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Mitogen-activated protein kinase 8 Ki = 3162.28 nM 5.5 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Death-associated protein kinase 3 Ki = 3981.07 nM 5.4 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Protein kinase C gamma type Ki = 3981.07 nM 5.4 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -

Data from ChEMBL 36 via Core Engine