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Compound Detail

CHEMBL217943

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O=C(NCc1ccccc1)c1ccc2cccnc2c1O

Basic Information

ChEMBL ID CHEMBL217943
Phase Preclinical
Structure Type MOL
InChI Key BMYUTWKKELIBCE-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

278.3
MW (Da)
2.87
ALogP
3
HBA
2
HBD
62.2
PSA (Ų)
0.77
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H14N2O2
MW 278.31
Aromatic Rings 3
Heavy Atoms 21
NP-Likeness -1.07

Activity Summary

EC50 1 meas. best 6.05
IC50 1 meas. best 5.38

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HEK293
CHEMBL614818
EC50 6.05 6.05 890.0 1
Egl nine homolog 1
CHEMBL5697
IC50 5.38 5.38 4200.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 22.77 uL.min-1.(10^6cells)-1 Rattus norvegicus
CL 49.0 mL.min-1.g-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
HEK293 EC50 = 890.0 nM 6.05 Induction of VEGF in HEK293 cells by ELISA 16931007
Egl nine homolog 1 IC50 = 4200.0 nM 5.38 Inhibition of human EGLN1 16931007

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL3301361 ADMET 3
16931007 10.1016/j.bmcl.2006.08.040 Egl nine homolog 1 1
16931007 10.1016/j.bmcl.2006.08.040 HEK293 1

Data from ChEMBL 36 via Core Engine