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Compound Detail

CHEMBL433493

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Oc1c(F)cc(Cn2cc[nH]c2=S)cc1F

Basic Information

ChEMBL ID CHEMBL433493
Phase Preclinical
Structure Type MOL
InChI Key UCQCUJWREUJRPA-UHFFFAOYSA-N
3
Targets
6
Activities
2
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

242.2
MW (Da)
2.58
ALogP
3
HBA
2
HBD
41.0
PSA (Ų)
0.79
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C10H8F2N2OS
MW 242.25
Aromatic Rings 2
Heavy Atoms 16
NP-Likeness -1.09

Activity Summary

IC50 5 meas. best 7.13
Ki 1 meas. best 8.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dopamine beta-hydroxylase
CHEMBL4702
Ki 8.24 8.24 5.7 1
Dopamine beta-hydroxylase
CHEMBL2992
IC50 7.13 7.13 74.1 1
Dopamine beta-hydroxylase
CHEMBL3102
IC50 7.13 7.13 74.1 2
Dopamine beta-hydroxylase
CHEMBL4702
IC50 7.13 7.13 74.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
3820219 10.1021/jm00386a008 Dopamine beta-hydroxylase 4
3820219 10.1021/jm00386a008 Rattus norvegicus 3
7783140 10.1021/jm00012a008 Dopamine beta-hydroxylase 1
3712378 10.1021/jm00156a002 Dopamine beta-hydroxylase 1
3712378 10.1021/jm00156a002 Unchecked 1
3712378 10.1021/jm00156a002 Rattus norvegicus 1
2296023 10.1021/jm00163a045 Dopamine beta-hydroxylase 1
2299645 10.1021/jm00164a051 Dopamine beta-hydroxylase 1
9435905 10.1021/jm970488n Dopamine beta-hydroxylase 1
3820219 10.1021/jm00386a008 No relevant target 1

Data from ChEMBL 36 via Core Engine