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Compound Detail

CHEMBL5439337

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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@](CN2CCN4CCOC[C@@H]4C2)(OC)/C(F)=C/C[C@H](C)C1)C[C@@]1(CCCc2cc(Cl)ccc21)CO3

Basic Information

ChEMBL ID CHEMBL5439337
Phase Preclinical
Structure Type MOL
InChI Key ZIQIEGUTYXQCOR-YDJVEDFVSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

924.5
MW (Da)
5.21
ALogP
13
HBA
1
HBD
149.3
PSA (Ų)
0.35
QED
3
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C46H59ClFN7O8S
MW 924.54
Aromatic Rings 3
Heavy Atoms 64
NP-Likeness -0.40

Activity Summary

Ki 1 meas. best 9.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Ki 9.77 9.77 0.2 1

Pharmacokinetic Data

Parameter Value Units Species
CL 7.7 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 = 0.17 nM 9.77 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 ADMET 5
37114951 10.1021/acs.jmedchem.2c01953 No relevant target 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