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Compound Detail

CHEMBL2000408

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Cc1cn2c(-c3ccnc(NCC(C)(C)CO)n3)c(-c3ccc(F)cc3F)nc2c(C)n1

Basic Information

ChEMBL ID CHEMBL2000408
Phase Preclinical
Structure Type MOL
InChI Key WIHAOLDOGQOGIU-UHFFFAOYSA-N
16
Targets
16
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

438.5
MW (Da)
4.18
ALogP
7
HBA
2
HBD
88.2
PSA (Ų)
0.47
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 C23H24F2N6O
MW 438.48
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -1.10

Activity Summary

Ki 16 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Casein kinase I isoform delta
CHEMBL2828
Ki 7.7 7.7 19.9 1
Mitogen-activated protein kinase 9
CHEMBL4179
Ki 7.3 7.3 50.1 1
Serine/threonine-protein kinase D3
CHEMBL2595
Ki 6.3 6.3 501.2 1
Casein kinase I isoform alpha
CHEMBL2793
Ki 6.1 6.1 794.3 1
Serine/threonine-protein kinase D2
CHEMBL4900
Ki 6.1 6.1 794.3 1
Casein kinase I isoform gamma-2
CHEMBL2543
Ki 5.8 5.8 1584.9 1
Mitogen-activated protein kinase kinase kinase kinase 5
CHEMBL4852
Ki 5.8 5.8 1584.9 1
Mitogen-activated protein kinase kinase kinase kinase 4
CHEMBL6166
Ki 5.8 5.8 1584.9 1
Mitogen-activated protein kinase 8
CHEMBL2276
Ki 5.7 5.7 1995.3 1
LIM domain kinase 1
CHEMBL3836
Ki 5.7 5.7 1995.3 1
Tyrosine-protein kinase FRK
CHEMBL4223
Ki 5.7 5.7 1995.3 1
Casein kinase I isoform gamma-1
CHEMBL2426
Ki 5.6 5.6 2511.9 1
Misshapen-like kinase 1
CHEMBL5518
Ki 5.6 5.6 2511.9 1
Glycogen synthase kinase-3 beta
CHEMBL262
Ki 5.5 5.5 3162.3 1
Serine/threonine-protein kinase TAO1
CHEMBL5261
Ki 5.5 5.5 3162.3 1
Casein kinase I isoform gamma-3
CHEMBL5084
Ki 5.4 5.4 3981.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Casein kinase I isoform delta Ki = 19.95 nM 7.7 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Mitogen-activated protein kinase 9 Ki = 50.12 nM 7.3 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Serine/threonine-protein kinase D3 Ki = 501.19 nM 6.3 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Serine/threonine-protein kinase D2 Ki = 794.33 nM 6.1 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Casein kinase I isoform alpha Ki = 794.33 nM 6.1 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Casein kinase I isoform gamma-2 Ki = 1584.89 nM 5.8 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Mitogen-activated protein kinase kinase kinase kinase 4 Ki = 1584.89 nM 5.8 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Mitogen-activated protein kinase kinase kinase kinase 5 Ki = 1584.89 nM 5.8 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Tyrosine-protein kinase FRK Ki = 1995.26 nM 5.7 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
LIM domain kinase 1 Ki = 1995.26 nM 5.7 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Mitogen-activated protein kinase 8 Ki = 1995.26 nM 5.7 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Casein kinase I isoform gamma-1 Ki = 2511.89 nM 5.6 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Misshapen-like kinase 1 Ki = 2511.89 nM 5.6 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Serine/threonine-protein kinase TAO1 Ki = 3162.28 nM 5.5 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Glycogen synthase kinase-3 beta Ki = 3162.28 nM 5.5 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Casein kinase I isoform gamma-3 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