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Compound Detail

CHEMBL5437473

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O=C(O)CNC(=O)c1ncc(C2CCN(S(=O)(=O)Cc3ccc(C(F)(F)F)cc3)CC2)cc1O

Basic Information

ChEMBL ID CHEMBL5437473
Phase Preclinical
Structure Type MOL
InChI Key WPVORGLHQMLTSW-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
2
Publications
0
Known Names

Molecular Properties

501.5
MW (Da)
2.33
ALogP
6
HBA
3
HBD
136.9
PSA (Ų)
0.53
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H22F3N3O6S
MW 501.48
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -1.16

Activity Summary

IC50 1 meas. best 7.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Egl nine homolog 1
CHEMBL5697
IC50 7.0 7.0 98.9 1

Pharmacokinetic Data

Parameter Value Units Species
CL 5.0 mL.min-1.g-1 Rattus norvegicus
T1/2 2.417 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Egl nine homolog 1 IC50 = 98.9 nM 7.0 Binding affinity to full length PHD2 (181 to 426 residues) (unknown origin) by f... 37367818

Literature References

PubMed DOI Target Context # Activities
37367818 10.1021/acs.jmedchem.3c00231 ADMET 2
37367818 10.1021/acs.jmedchem.3c00231 Egl nine homolog 1 1

Data from ChEMBL 36 via Core Engine