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Compound Detail

CHEMBL5440375

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COc1nn(C)cc1C(=O)N[S@]1(=O)=NC(=O)c2ccc3c(c2)N(C[C@@H]2CCO[C@H]2[C@@H](OC)/C(F)=C/C[C@H](C)C1)C[C@@]1(CCCc2cc(Cl)ccc21)CO3

Basic Information

ChEMBL ID CHEMBL5440375
Phase Preclinical
Structure Type MOL
InChI Key VFFBTCWSTVFCJE-XGXMSZIGSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

770.3
MW (Da)
5.82
ALogP
10
HBA
1
HBD
133.6
PSA (Ų)
0.35
QED
2
Ro5 Violations
4
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C38H45ClFN5O7S
MW 770.32
Aromatic Rings 3
Heavy Atoms 53
NP-Likeness -0.23

Activity Summary

Ki 1 meas. best 9.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Ki 9.6 9.6 0.2 1

Pharmacokinetic Data

Parameter Value Units Species
CL 16.0 mL.min-1.g-1 Homo sapiens
CL 9.3 mL.min-1.g-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked Ki = 0.25 nM 9.6 Inhibition of terbium-labelled Mcl-1 (unknown origin)/Bim BH3 peptide (H3N-(C/Cy... 37114951

Literature References

PubMed DOI Target Context # Activities
37114951 10.1021/acs.jmedchem.2c01953 No relevant target 4
37114951 10.1021/acs.jmedchem.2c01953 ADMET 4
37114951 10.1021/acs.jmedchem.2c01953 Unchecked 1
37114951 10.1021/acs.jmedchem.2c01953 MOLP-8 1

Data from ChEMBL 36 via Core Engine