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Compound Detail

CHEMBL4090599

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COC[C@H]1CN(Cc2ccccn2)C(=O)[C@@H]2CCC[C@H]1N2S(=O)(=O)c1cc(Cl)cc(Cl)c1

Basic Information

ChEMBL ID CHEMBL4090599
Phase Preclinical
Structure Type MOL
InChI Key CLJZLDBGGLGZDB-LPTQZCDUSA-N
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

498.4
MW (Da)
3.61
ALogP
5
HBA
0
HBD
79.8
PSA (Ų)
0.61
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H25Cl2N3O4S
MW 498.43
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -0.91

Activity Summary

Ki 6 meas. best 9.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Peptidyl-prolyl cis-trans isomerase FKBP1A
CHEMBL1902
Ki 9.35 9.35 0.5 1
Peptidyl-prolyl cis-trans isomerase FKBP1B
CHEMBL2430
Ki 8.91 8.91 1.2 1
Peptidyl-prolyl cis-trans isomerase FKBP4
CHEMBL4050
Ki 7.72 7.72 18.9 1
Peptidyl-prolyl cis-trans isomerase FKBP5
CHEMBL2052031
Ki 7.61 7.61 24.5 1
Peptidyl-prolyl cis-trans isomerase FKBP2
CHEMBL4105949
Ki 7.22 7.22 60.5 1
Peptidyl-prolyl cis-trans isomerase FKBP3
CHEMBL4746
Ki 5.95 5.95 1133.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29578710 10.1021/acs.jmedchem.8b00137 Peptidyl-prolyl cis-trans isomerase FKBP1A 1
29578710 10.1021/acs.jmedchem.8b00137 Peptidyl-prolyl cis-trans isomerase FKBP1B 1
29578710 10.1021/acs.jmedchem.8b00137 Peptidyl-prolyl cis-trans isomerase FKBP2 1
29578710 10.1021/acs.jmedchem.8b00137 Peptidyl-prolyl cis-trans isomerase FKBP3 1
29578710 10.1021/acs.jmedchem.8b00137 Peptidyl-prolyl cis-trans isomerase FKBP5 1
29578710 10.1021/acs.jmedchem.8b00137 Peptidyl-prolyl cis-trans isomerase FKBP4 1

Data from ChEMBL 36 via Core Engine