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Compound Detail

CHEMBL3799292

(R)-9s
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C[C@H](c1cccc(C#N)c1)n1cc(Cl)cc(C(N)=O)c1=N

Basic Information

ChEMBL ID CHEMBL3799292
Name (R)-9s
Phase Preclinical
Structure Type MOL
InChI Key CDJPHTNUARAVMH-SECBINFHSA-N

Known Names

Tp-009
2
Targets
3
Activities
2
Assay Types
5
PK Parameters
20
Publications
1
Known Names

Molecular Properties

300.8
MW (Da)
2.20
ALogP
4
HBA
2
HBD
95.7
PSA (Ų)
0.91
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug Chemical Probe

Extended Properties

Molecular Formula C15H13ClN4O
MW 300.75
Aromatic Rings 2
Heavy Atoms 21
NP-Likeness -1.40

Activity Summary

Ki 2 meas. best 8.8
IC50 1 meas. best 5.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1D adrenergic receptor
CHEMBL223
Ki 8.8 8.8 1.6 2
Alpha-2B adrenergic receptor
CHEMBL1942
IC50 5.85 5.85 1400.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 368.0 ng.hr.mL-1 Rattus norvegicus
CL 39.17 mL.min-1.kg-1 Rattus norvegicus
Cmax 472.15 nM Rattus norvegicus
F 86.0 % Rattus norvegicus
MRT 3.14 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL4507301 Tyrosine-protein kinase ABL1 15
- 10.6019/CHEMBL4507301 Epidermal growth factor receptor 12
- 10.6019/CHEMBL4507301 Receptor-type tyrosine-protein kinase FLT3 11
- 10.6019/CHEMBL4507301 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 10
26954848 10.1021/acs.jmedchem.5b01528 Rattus norvegicus 9
- 10.6019/CHEMBL4507301 Mast/stem cell growth factor receptor Kit 9
- 10.6019/CHEMBL4507301 Unchecked 8
- 10.6019/CHEMBL4507301 Proto-oncogene tyrosine-protein kinase receptor Ret 4
- 10.6019/CHEMBL4507301 ALK tyrosine kinase receptor 3
- 10.6019/CHEMBL4507301 Alpha-1D adrenergic receptor 3
- 10.6019/CHEMBL4507301 Hepatocyte growth factor receptor 3
- 10.6019/CHEMBL4507301 Beta-3 adrenergic receptor 2
- 10.6019/CHEMBL4507301 Tyrosine-protein kinase JAK1 2
- 10.6019/CHEMBL4507301 Beta-2 adrenergic receptor 2
- 10.6019/CHEMBL4507301 Beta-1 adrenergic receptor 2
- 10.6019/CHEMBL4507301 Alpha-2B adrenergic receptor 2
- 10.6019/CHEMBL4507301 Macrophage colony-stimulating factor 1 receptor 2
- 10.6019/CHEMBL4507301 Alpha-2A adrenergic receptor 2
26954848 10.1021/acs.jmedchem.5b01528 Urinary bladder 2
26954848 10.1021/acs.jmedchem.5b01528 Unchecked 2

Data from ChEMBL 36 via Core Engine