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Compound Detail

CHEMBL2001998

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CNC(=O)N1CCN(CCCOc2ccc3c(c2)-c2[nH]nc(-c4ccc(C#N)nc4)c2C3)CC1

Basic Information

ChEMBL ID CHEMBL2001998
Phase Preclinical
Structure Type MOL
InChI Key YGJKHDBRTOPTNK-UHFFFAOYSA-N
11
Targets
11
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

457.5
MW (Da)
2.64
ALogP
6
HBA
2
HBD
110.2
PSA (Ų)
0.43
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 C25H27N7O2
MW 457.54
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.34

Activity Summary

Ki 11 meas. best 7.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aurora kinase B
CHEMBL2185
Ki 7.3 7.3 50.1 1
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
Ki 7.0 7.0 100.0 1
Serine/threonine-protein kinase MARK2
CHEMBL3831
Ki 6.6 6.6 251.2 1
Macrophage colony-stimulating factor 1 receptor
CHEMBL1844
Ki 6.4 6.4 398.1 1
MAP/microtubule affinity-regulating kinase 3
CHEMBL5600
Ki 6.4 6.4 398.1 1
Tyrosine-protein kinase ITK/TSK
CHEMBL2959
Ki 6.3 6.3 501.2 1
Aurora kinase A
CHEMBL4722
Ki 6.2 6.2 631.0 1
Serine/threonine-protein kinase Chk2
CHEMBL2527
Ki 6.1 6.1 794.3 1
Tyrosine-protein kinase Lck
CHEMBL258
Ki 5.9 5.9 1258.9 1
Vascular endothelial growth factor receptor 2
CHEMBL279
Ki 5.7 5.7 1995.3 1
Fibroblast growth factor receptor 1
CHEMBL3650
Ki 5.5 5.5 3162.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Aurora kinase B Ki = 50.12 nM 7.3 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Receptor-type tyrosine-protein kinase FLT3 Ki = 100.0 nM 7.0 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Serine/threonine-protein kinase MARK2 Ki = 251.19 nM 6.6 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Macrophage colony-stimulating factor 1 receptor Ki = 398.11 nM 6.4 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
MAP/microtubule affinity-regulating kinase 3 Ki = 398.11 nM 6.4 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Tyrosine-protein kinase ITK/TSK Ki = 501.19 nM 6.3 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Aurora kinase A Ki = 630.96 nM 6.2 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... -
Tyrosine-protein kinase Lck Ki = 1258.93 nM 5.9 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Vascular endothelial growth factor receptor 2 Ki = 1995.26 nM 5.7 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Fibroblast growth factor receptor 1 Ki = 3162.28 nM 5.5 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -

Data from ChEMBL 36 via Core Engine