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Compound Detail

CHEMBL3962241

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COc1cc(F)ccc1-c1nc(Nc2cc(F)cc(CS(C)(=N)=O)c2)ncc1F

Basic Information

ChEMBL ID CHEMBL3962241
Phase Preclinical
Structure Type MOL
InChI Key NSJOYQIOHVHMCZ-UHFFFAOYSA-N
6
Targets
14
Activities
1
Assay Types
5
PK Parameters
18
Publications
0
Known Names

Molecular Properties

422.4
MW (Da)
4.49
ALogP
6
HBA
2
HBD
88.0
PSA (Ų)
0.61
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 C19H17F3N4O2S
MW 422.43
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.38

Activity Summary

IC50 14 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 9
CHEMBL3116
IC50 8.3 7.91 5.0 6
CDK9/cyclin T1
CHEMBL2111389
IC50 7.43 7.43 37.0 1
A2780
CHEMBL614004
IC50 7.24 7.215 57.0 2
MOLM-13
CHEMBL3706572
IC50 7.07 7.07 85.0 1
Cyclin-dependent kinase 2
CHEMBL301
IC50 6.66 6.5567 220.0 3
Cyclin-dependent kinase 2/cyclin E1
CHEMBL1907605
IC50 5.4 5.4 3959.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 28.33 mL.min-1.kg-1 Rattus norvegicus
CL 31.67 mL.min-1.kg-1 Rattus norvegicus
CL 26.67 mL.min-1.kg-1 Rattus norvegicus
CL 21.67 mL.min-1.kg-1 Rattus norvegicus
T1/2 1.0 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 9 IC50 = 5.0 nM 8.3 CDK9/CycT1 Kinase Assay: Recombinant full-length His-tagged human CDK9 and CycT1... -
Cyclin-dependent kinase 9 IC50 = 6.0 nM 8.22 CDK9/CycT1 Kinase Assay: Recombinant full-length His-tagged human CDK9 and CycT1... -
Cyclin-dependent kinase 9 IC50 = 9.0 nM 8.05 CDK9/CycT1 Kinase Assay: Recombinant full-length His-tagged human CDK9 and CycT1... -
Cyclin-dependent kinase 9 IC50 = 13.0 nM 7.89 CDK9/CycT1 : Recombinant full-length His-tagged human CDK9 and CycT1, expressed ... -
Cyclin-dependent kinase 9 IC50 = 27.0 nM 7.57 CDK9/CycT1 : Recombinant full-length His-tagged human CDK9 and CycT1, expressed ... -
Cyclin-dependent kinase 9 IC50 = 37.0 nM 7.43 CDK9/CycT1 : Recombinant full-length His-tagged human CDK9 and CycT1, expressed ... -
CDK9/cyclin T1 IC50 = 37.0 nM 7.43 Inhibition of recombinant full length His-tagged human CDK9/cyclin T1 expressed ... 32870008
A2780 IC50 = 57.0 nM 7.24 Antiproliferative activity against human A2780 cells assessed as inhibition of c... 34264057
A2780 IC50 = 64.0 nM 7.19 Antiproliferative activity against human A2780 cells assessed as inhibition of c... 34264057
MOLM-13 IC50 = 85.0 nM 7.07 Antiproliferative activity against human MOLM-13 cells assessed as inhibition of... 34264057
Cyclin-dependent kinase 2 IC50 = 220.0 nM 6.66 CDK2/CycE Kinase Assay: Recombinant fusion proteins of GST and human CDK2 and of... -
Cyclin-dependent kinase 2 IC50 = 310.0 nM 6.51 CDK2/CycE Kinase Assay: Recombinant fusion proteins of GST and human CDK2 and of... -
Cyclin-dependent kinase 2 IC50 = 320.0 nM 6.5 CDK2/CycE Kinase Assay: Recombinant fusion proteins of GST and human CDK2 and of... -
Cyclin-dependent kinase 2/cyclin E1 IC50 = 3959.0 nM 5.4 Inhibition of recombinant GST-tagged human CDK2/GST-tagged cyclin E expressed in... 32870008

Literature References

Data from ChEMBL 36 via Core Engine