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Compound Detail

CHEMBL1761577

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Cn1cc(-c2ccc3cnc(Nc4ccc(-n5cnc(N6CCOCC6)n5)cc4)nc3c2Cl)cn1

Basic Information

ChEMBL ID CHEMBL1761577
Phase Preclinical
Structure Type MOL
InChI Key GIIITGYQMLZQJE-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
6
PK Parameters
6
Publications
0
Known Names

Molecular Properties

488.0
MW (Da)
3.84
ALogP
10
HBA
1
HBD
98.8
PSA (Ų)
0.40
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H22ClN9O
MW 487.96
Aromatic Rings 5
Heavy Atoms 35
NP-Likeness -1.85

Activity Summary

IC50 2 meas. best 7.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 10
CHEMBL2637
IC50 7.4 7.4 40.0 1
Transcription factor Jun
CHEMBL4977
IC50 7.0 7.0 100.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 1122.31 ng.hr.mL-1 Rattus norvegicus
CL 6.0 mL.min-1.kg-1 Rattus norvegicus
Cmax 300.0 nM Rattus norvegicus
F 19.0 % Rattus norvegicus
T1/2 3.0 hr Rattus norvegicus
Vd 1.4 l Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Mitogen-activated protein kinase 10 IC50 = 40.0 nM 7.4 Inhibition of JNK3 by HRTF 21316221
Transcription factor Jun IC50 = 100.0 nM 7.0 Inhibition of c-Jun 21316221

Literature References

PubMed DOI Target Context # Activities
21316221 10.1016/j.bmcl.2011.01.079 Rattus norvegicus 6
21316221 10.1016/j.bmcl.2011.01.079 Mitogen-activated protein kinase 10 1
21316221 10.1016/j.bmcl.2011.01.079 Transcription factor Jun 1
21316221 10.1016/j.bmcl.2011.01.079 Plasma 1
21316221 10.1016/j.bmcl.2011.01.079 Brain 1
21316221 10.1016/j.bmcl.2011.01.079 Unchecked 1

Data from ChEMBL 36 via Core Engine