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Compound Detail

CHEMBL421980

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COc1cc2c(cc1OC)CN(CCn1c(-c3ccc(N(C)C)cc3)nc3ccccc3c1=O)CC2

Basic Information

ChEMBL ID CHEMBL421980
Phase Preclinical
Structure Type MOL
InChI Key HSFNWCVLEHOTNA-UHFFFAOYSA-N
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

484.6
MW (Da)
4.21
ALogP
7
HBA
0
HBD
59.8
PSA (Ų)
0.39
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H32N4O3
MW 484.60
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -1.03

Activity Summary

EC50 2 meas. best 5.52
IC50 2 meas. best 5.98

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Multidrug resistance-associated protein 1
CHEMBL3004
IC50 5.98 5.98 1050.0 1
ATP-dependent translocase ABCB1
CHEMBL3467
IC50 5.97 5.97 1070.0 1
Unchecked
CHEMBL612545
EC50 5.52 5.52 3010.0 1
EMT6
CHEMBL614294
EC50 5.48 5.48 3300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11844674 10.1016/s0960-894x(01)00804-6 ATP-dependent translocase ABCB1 1
11844674 10.1016/s0960-894x(01)00804-6 Multidrug resistance-associated protein 1 1
11844674 10.1016/s0960-894x(01)00804-6 EMT6 1
11844674 10.1016/s0960-894x(01)00804-6 Unchecked 1

Data from ChEMBL 36 via Core Engine