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Compound Detail

CHEMBL496851

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CN1C[C@@H]2CN(c3ccc(-c4ccc5[nH]ccc5c4)nn3)C[C@@H]2C1.Cc1ccc(S(=O)(=O)O)cc1

Basic Information

ChEMBL ID CHEMBL496851
Phase Preclinical
Structure Type MOL
InChI Key ZSZAAIMFYZCLFR-FAESNJTISA-N
Parent Compound CHEMBL1187288
Active Moiety CHEMBL1187288
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

319.4
MW (Da)
2.62
ALogP
4
HBA
1
HBD
48.0
PSA (Ų)
0.79
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H29N5O3S
MW 491.62
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -1.13

Activity Summary

EC50 1 meas. best 6.5
Ki 1 meas. best 9.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neuronal acetylcholine receptor subunit alpha-7
CHEMBL4980
Ki 9.62 9.62 0.2 1
Neuronal acetylcholine receptor subunit alpha-7
CHEMBL2492
EC50 6.5 6.5 320.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19552432 10.1021/jm900249k Neuronal acetylcholine receptor subunit alpha-7 3
19552432 10.1021/jm900249k Neuronal acetylcholine receptor; alpha4/beta2 3
19552432 10.1021/jm900249k Unchecked 1

Data from ChEMBL 36 via Core Engine