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Compound Detail

CHEMBL3793424

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Cc1c(-c2ccc(N3CCc4cccc(C(=O)Nc5nc6ccccc6s5)c4C3)nc2C(=O)O)cnn1CC12CC3CC(CC(C3)C1)C2

Basic Information

ChEMBL ID CHEMBL3793424
Phase Preclinical
Structure Type MOL
InChI Key QCQQONWEDCOTBV-UHFFFAOYSA-N
5
Targets
8
Activities
2
Assay Types
12
PK Parameters
20
Publications
0
Known Names

Molecular Properties

658.8
MW (Da)
7.59
ALogP
8
HBA
2
HBD
113.2
PSA (Ų)
0.19
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C38H38N6O3S
MW 658.83
Aromatic Rings 5
Heavy Atoms 48
NP-Likeness -1.34

Activity Summary

Ki 5 meas. best 8.4
EC50 3 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bcl-2-like protein 2
CHEMBL4677
Ki 8.4 8.4 4.0 1
NON-PROTEIN TARGET
CHEMBL3879801
EC50 8.22 8.22 6.0 1
Apoptosis regulator Bcl-2
CHEMBL4860
Ki 8.22 8.2167 6.0 3
MOLT-4
CHEMBL614177
EC50 8.22 8.21 6.0 2
Induced myeloid leukemia cell differentiation protein Mcl-1
CHEMBL4361
Ki 6.85 6.85 142.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 62522.97 ng.hr.mL-1 Rattus norvegicus
AUC 8235.38 ng.hr.mL-1 Rattus norvegicus
AUC 22729.64 ng.hr.mL-1 Mus musculus
AUC 2510.14 ng.hr.mL-1 Mus musculus
CL 1.333 mL.min-1.kg-1 Rattus norvegicus
CL 3.667 mL.min-1.kg-1 Mus musculus
Cmax 1970.0 nM Rattus norvegicus
Cmax 1460.0 nM Mus musculus
F 13.0 % Rattus norvegicus
F 11.0 % Mus musculus
T1/2 3.9 hr Rattus norvegicus
T1/2 2.4 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

Data from ChEMBL 36 via Core Engine