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Compound Detail

CHEMBL291398

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O=c1c(I)cc(I)c2n1CC1CNCC2C1

Basic Information

ChEMBL ID CHEMBL291398
Phase Preclinical
Structure Type MOL
InChI Key PZHBDNKGVXGCFL-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

442.0
MW (Da)
1.76
ALogP
3
HBA
1
HBD
34.0
PSA (Ų)
0.62
QED
0
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C11H12I2N2O
MW 442.04
Aromatic Rings 1
Heavy Atoms 16
NP-Likeness -0.09

Activity Summary

EC50 1 meas. best 7.38
Ki 1 meas. best 9.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neuronal acetylcholine receptor; alpha4/beta2
CHEMBL1907596
Ki 9.28 9.28 0.5 1
Neuronal acetylcholine receptor; alpha4/beta2
CHEMBL1907589
EC50 7.38 7.38 42.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15686946 10.1016/j.bmcl.2004.11.073 Neuronal acetylcholine receptor; alpha3/beta4 3
15686946 10.1016/j.bmcl.2004.11.073 Neuronal acetylcholine receptor; alpha4/beta2 3
15686946 10.1016/j.bmcl.2004.11.073 Acetylcholine receptor; alpha1/beta1/delta/gamma 2
12747776 10.1021/jm020859m Neuronal acetylcholine receptor; alpha4/beta2 1

Data from ChEMBL 36 via Core Engine