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Compound Detail

CHEMBL4513768

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CCN1CCN(c2cc(Nc3ncc(-c4ccncc4)s3)nc(C)n2)CC1.Cl

Basic Information

ChEMBL ID CHEMBL4513768
Phase Preclinical
Structure Type MOL
InChI Key SNLQNYOOKITUPG-UHFFFAOYSA-N
Parent Compound CHEMBL4596788
Active Moiety CHEMBL4596788
4
Targets
8
Activities
1
Assay Types
14
PK Parameters
20
Publications
0
Known Names

Molecular Properties

381.5
MW (Da)
3.19
ALogP
8
HBA
1
HBD
70.1
PSA (Ų)
0.73
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H24ClN7S
MW 417.97
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -2.16

Activity Summary

IC50 8 meas. best 10.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 10.0 8.904 0.1 5
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
IC50 8.52 8.52 3.0 1
High affinity nerve growth factor receptor
CHEMBL2815
IC50 8.31 8.31 4.9 1
Mast/stem cell growth factor receptor Kit
CHEMBL1936
IC50 7.25 7.25 56.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 804.0 ng.hr.mL-1 Rattus norvegicus
AUC 1470.0 ng.hr.mL-1 Rattus norvegicus
AUC 542.0 ng.hr.mL-1 Mus musculus
AUC 1955.0 ng.hr.mL-1 Mus musculus
CL 39.6 mL.min-1.kg-1 Rattus norvegicus
CL 70.7 mL.min-1.kg-1 Mus musculus
Cmax 401.04 nM Rattus norvegicus
Cmax 851.88 nM Mus musculus
F 36.0 % Rattus norvegicus
F 68.0 % Mus musculus
T1/2 5.7 hr Rattus norvegicus
T1/2 3.9 hr Rattus norvegicus
T1/2 1.6 hr Mus musculus
T1/2 4.1 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31721578 10.1021/acs.jmedchem.9b01229 Mast/stem cell growth factor receptor Kit 41
31721578 10.1021/acs.jmedchem.9b01229 ADMET 18
31721578 10.1021/acs.jmedchem.9b01229 Unchecked 9
31721578 10.1021/acs.jmedchem.9b01229 Receptor-type tyrosine-protein kinase FLT3 8
31721578 10.1021/acs.jmedchem.9b01229 MOLM-13 5
31721578 10.1021/acs.jmedchem.9b01229 GIST430 4
31721578 10.1021/acs.jmedchem.9b01229 Kasumi 1 4
31721578 10.1021/acs.jmedchem.9b01229 Platelet-derived growth factor receptor alpha 3
31721578 10.1021/acs.jmedchem.9b01229 Proto-oncogene tyrosine-protein kinase Src 2
31721578 10.1021/acs.jmedchem.9b01229 High affinity nerve growth factor receptor 2
31721578 10.1021/acs.jmedchem.9b01229 Mus musculus 2
31721578 10.1021/acs.jmedchem.9b01229 GISTT1 1
31721578 10.1021/acs.jmedchem.9b01229 K562 1
31721578 10.1021/acs.jmedchem.9b01229 U-937 1
31721578 10.1021/acs.jmedchem.9b01229 RS4-11 1
31721578 10.1021/acs.jmedchem.9b01229 MV4-11 1
31721578 10.1021/acs.jmedchem.9b01229 GIST48 1
31721578 10.1021/acs.jmedchem.9b01229 GIST882 1
31721578 10.1021/acs.jmedchem.9b01229 Platelet-derived growth factor receptor beta 1
31721578 10.1021/acs.jmedchem.9b01229 BDNF/NT-3 growth factors receptor 1

Data from ChEMBL 36 via Core Engine