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Compound Detail

CHEMBL5183986

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CCNC(=O)c1noc(-c2cc(-c3cccc(C(C)C)c3)c(O)cc2O)c1-c1ccc(CN2CCOCC2)cc1

Basic Information

ChEMBL ID CHEMBL5183986
Phase Preclinical
Structure Type MOL
InChI Key BEZRWPZSNISNFG-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
4
Publications
0
Known Names

Molecular Properties

541.6
MW (Da)
5.79
ALogP
7
HBA
3
HBD
108.1
PSA (Ų)
0.26
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H35N3O5
MW 541.65
Aromatic Rings 4
Heavy Atoms 40
NP-Likeness -0.73

Activity Summary

Kd 1 meas. best 6.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Kd 6.32 6.32 476.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 0.0919 mL.min-1.kg-1 Homo sapiens
CL 0.0827 mL.min-1.kg-1 Homo sapiens
T1/2 0.2517 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked Kd = 476.0 nM 6.32 Binding affinity to recombinant Candida albicans Hsp90 NBD expressed in Escheric... 35298171

Literature References

PubMed DOI Target Context # Activities
35298171 10.1021/acs.jmedchem.1c01991 Candida albicans 6
35298171 10.1021/acs.jmedchem.1c01991 ADMET 4
35298171 10.1021/acs.jmedchem.1c01991 Unchecked 1
35298171 10.1021/acs.jmedchem.1c01991 Heat shock protein HSP90 1

Data from ChEMBL 36 via Core Engine