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Compound Detail

CHEMBL133987

TRIMELAMOL
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CN(CO)c1nc(N(C)CO)nc(N(C)CO)n1

Basic Information

ChEMBL ID CHEMBL133987
Name TRIMELAMOL
Phase Preclinical
Structure Type MOL
InChI Key MHVFYGIQJNFWGQ-UHFFFAOYSA-N
4
Targets
6
Activities
1
Assay Types
5
PK Parameters
8
Publications
0
Known Names

Molecular Properties

258.3
MW (Da)
-1.97
ALogP
9
HBA
3
HBD
109.1
PSA (Ų)
0.50
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 C9H18N6O3
MW 258.28
Aromatic Rings 1
Heavy Atoms 18
NP-Likeness -0.35

Activity Summary

IC50 6 meas. best 5.07

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NCI-H69
CHEMBL614805
IC50 5.07 5.07 8500.0 1
NON-PROTEIN TARGET
CHEMBL3879801
IC50 5.03 4.7167 9400.0 3
PC-6
CHEMBL614235
IC50 4.89 4.89 12900.0 1
L1210
CHEMBL386
IC50 4.48 4.48 33400.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 2.0 hr -
T1/2 3.333 hr -
T1/2 13.67 hr -
T1/2 4.583 hr -
T1/2 5.833 hr -

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
8277501 10.1021/jm00078a008 ADMET 5
8277501 10.1021/jm00078a008 NON-PROTEIN TARGET 3
8277501 10.1021/jm00078a008 PC-6 1
8277501 10.1021/jm00078a008 NCI-H69 1
8277501 10.1021/jm00078a008 L1210 1
8277501 10.1021/jm00078a008 No relevant target 1
18834112 10.1021/jm800656v Amine oxidase [flavin-containing] A 1
18834112 10.1021/jm800656v Amine oxidase [flavin-containing] B 1

Data from ChEMBL 36 via Core Engine