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Compound Detail

CHEMBL4087666

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Cc1ccc(NC(=O)c2ccc3c(c2)OCCO3)cc1NC(=O)c1ccc2nc(OCCN3CCCC3)ccc2c1

Basic Information

ChEMBL ID CHEMBL4087666
Phase Preclinical
Structure Type MOL
InChI Key KLHOCHQJHXNKAS-UHFFFAOYSA-N
3
Targets
10
Activities
3
Assay Types
21
PK Parameters
20
Publications
0
Known Names

Molecular Properties

552.6
MW (Da)
5.29
ALogP
7
HBA
2
HBD
102.0
PSA (Ų)
0.31
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug Chemical Probe

Extended Properties

Molecular Formula C32H32N4O5
MW 552.63
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -1.54

Activity Summary

IC50 7 meas. best 7.73
Kd 2 meas. best 7.36
Ki 1 meas. best 7.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Heat shock factor protein 1
CHEMBL5869
IC50 7.73 7.5625 18.6 4
Pirin
CHEMBL2010627
Ki 7.55 7.55 28.0 1
Pirin
CHEMBL2010627
IC50 7.48 7.48 33.0 2
Pirin
CHEMBL2010627
Kd 7.36 7.36 43.6 2
Serine/threonine-protein kinase B-raf
CHEMBL5145
IC50 5.54 5.54 2900.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 3205.25 ng.hr.mL-1 Mus musculus
AUC 1050.0 ng.hr.mL-1 Mus musculus
CL 23.0 mL.min-1.g-1 Mus musculus
CL 9.2 mL.min-1.kg-1 Mus musculus
CL 1100.0 mL.min-1.kg-1 Mus musculus
CL 10.0 % Mus musculus
CL 20.0 mL.min-1.kg-1 Rattus norvegicus
CL 72.0 mL.min-1.g-1 Homo sapiens
CL 1100.0 mL.min-1.kg-1 Rattus norvegicus
CL 0.023 mL.min-1.kg-1 Mus musculus
CL 20.0 mL.min-1.g-1 Rattus norvegicus
F 39.0 % Mus musculus
F 11.0 % Rattus norvegicus
Fu 0.0083 - Mus musculus
Fu 0.015 - Mus musculus
Fu 0.47 - Homo sapiens
Fu 0.01 - Mus musculus
Fu 0.025 - Mus musculus
Fu 0.019 - Rattus norvegicus
T1/2 5.3 hr Mus musculus
Vd 510.0 L.kg-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

Data from ChEMBL 36 via Core Engine