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Compound Detail

CHEMBL452776

CELTISINE
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COc1cc2c(cc1O)Oc1c(O)ccc3c1[C@H](C2)N(C)CC3

Basic Information

ChEMBL ID CHEMBL452776
Name CELTISINE
Phase Preclinical
Structure Type MOL
InChI Key VRFVDWALYCNYTM-LBPRGKRZSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

313.4
MW (Da)
2.98
ALogP
5
HBA
2
HBD
62.2
PSA (Ų)
0.85
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C18H19NO4
MW 313.35
Aromatic Rings 2
Heavy Atoms 23
NP-Likeness 1.65

Activity Summary

IC50 4 meas. best 7.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(2) dopamine receptor
CHEMBL217
IC50 7.52 7.52 30.0 1
D(2) dopamine receptor
CHEMBL339
IC50 7.52 7.52 30.0 1
D(1A) dopamine receptor
CHEMBL2056
IC50 7.22 7.22 60.0 1
D(1A) dopamine receptor
CHEMBL265
IC50 7.22 7.22 60.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
8676127 10.1021/np50124a001 Unchecked 2
17228858 10.1021/jm060959i D(1A) dopamine receptor 1
17228858 10.1021/jm060959i D(2) dopamine receptor 1
17228858 10.1021/jm060959i Sodium-dependent dopamine transporter 1
8676127 10.1021/np50124a001 Sodium-dependent dopamine transporter 1
39038276 10.1021/acs.jmedchem.4c00537 D(1A) dopamine receptor 1
39038276 10.1021/acs.jmedchem.4c00537 D(2) dopamine receptor 1

Data from ChEMBL 36 via Core Engine