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Compound Detail

CHEMBL1999749

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COc1cc(Nc2ncnc3ccc(-c4ccc(CN5CC6C(CO)C6C5)cc4)cc23)ccc1Oc1ccccc1

Basic Information

ChEMBL ID CHEMBL1999749
Phase Preclinical
Structure Type MOL
InChI Key WZZXMNBOPNKKSX-UHFFFAOYSA-N
13
Targets
13
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

544.7
MW (Da)
6.51
ALogP
7
HBA
2
HBD
79.7
PSA (Ų)
0.22
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H32N4O3
MW 544.66
Aromatic Rings 5
Heavy Atoms 41
NP-Likeness -0.62

Activity Summary

Ki 13 meas. best 8.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Receptor tyrosine-protein kinase erbB-2
CHEMBL1824
Ki 8.8 8.8 1.6 1
Tyrosine-protein kinase Fyn
CHEMBL1841
Ki 8.6 8.6 2.5 1
Epidermal growth factor receptor
CHEMBL203
Ki 8.2 8.2 6.3 1
Tyrosine-protein kinase Blk
CHEMBL2250
Ki 7.9 7.9 12.6 1
Receptor tyrosine-protein kinase erbB-4
CHEMBL3009
Ki 7.8 7.8 15.8 1
Tyrosine-protein kinase Lyn
CHEMBL3905
Ki 7.2 7.2 63.1 1
Tyrosine-protein kinase Lck
CHEMBL258
Ki 6.5 6.5 316.2 1
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
Ki 6.4 6.4 398.1 1
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
Ki 6.3 6.3 501.2 1
Serine/threonine-protein kinase D2
CHEMBL4900
Ki 6.3 6.3 501.2 1
Serine/threonine-protein kinase Chk2
CHEMBL2527
Ki 5.9 5.9 1258.9 1
Protein kinase C delta type
CHEMBL2996
Ki 5.6 5.6 2511.9 1
Protein kinase C gamma type
CHEMBL2938
Ki 5.1 5.1 7943.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Receptor tyrosine-protein kinase erbB-2 Ki = 1.585 nM 8.8 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Tyrosine-protein kinase Fyn Ki = 2.512 nM 8.6 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Epidermal growth factor receptor Ki = 6.31 nM 8.2 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Tyrosine-protein kinase Blk Ki = 12.59 nM 7.9 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Receptor tyrosine-protein kinase erbB-4 Ki = 15.85 nM 7.8 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Tyrosine-protein kinase Lyn Ki = 63.1 nM 7.2 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Tyrosine-protein kinase Lck Ki = 316.23 nM 6.5 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Proto-oncogene tyrosine-protein kinase Src Ki = 398.11 nM 6.4 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Serine/threonine-protein kinase D2 Ki = 501.19 nM 6.3 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Receptor-type tyrosine-protein kinase FLT3 Ki = 501.19 nM 6.3 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Serine/threonine-protein kinase Chk2 Ki = 1258.93 nM 5.9 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Protein kinase C delta type Ki = 2511.89 nM 5.6 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Protein kinase C gamma type Ki = 7943.28 nM 5.1 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -

Data from ChEMBL 36 via Core Engine