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Compound Detail

CHEMBL5426438

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CO[C@H]1/C(F)=C/C[C@H](C)[C@@H](C)S(=O)(=O)NC(=O)c2cnc3c(n2)N(C[C@@H]2CCO[C@H]21)C[C@@]1(CCCc2cc(Cl)ccc21)CO3

Basic Information

ChEMBL ID CHEMBL5426438
Phase Preclinical
Structure Type MOL
InChI Key NXZDUGDBNWJJHK-AJQIFTSWSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

649.2
MW (Da)
4.36
ALogP
9
HBA
1
HBD
120.0
PSA (Ų)
0.48
QED
1
Ro5 Violations
1
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H38ClFN4O6S
MW 649.18
Aromatic Rings 2
Heavy Atoms 44
NP-Likeness 0.22

Activity Summary

Ki 1 meas. best 8.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Ki 8.28 8.28 5.3 1

Pharmacokinetic Data

Parameter Value Units Species
CL 98.0 mL.min-1.g-1 Homo sapiens
CL 7.7 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 = 5.29 nM 8.28 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 2
37114951 10.1021/acs.jmedchem.2c01953 Unchecked 1
37114951 10.1021/acs.jmedchem.2c01953 MOLP-8 1

Data from ChEMBL 36 via Core Engine