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Compound Detail

CHEMBL37061

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Nc1nc(N)c2c(Cl)c(CNc3ccc(C(=O)NC(CCC(=O)O)C(=O)O)cc3)ccc2n1

Basic Information

ChEMBL ID CHEMBL37061
Phase Preclinical
Structure Type MOL
InChI Key PFAJRSFHQCUKQB-UHFFFAOYSA-N
6
Targets
7
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

472.9
MW (Da)
2.11
ALogP
8
HBA
6
HBD
193.6
PSA (Ų)
0.27
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H21ClN6O5
MW 472.89
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.60

Activity Summary

IC50 7 meas. best 8.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HuTu80
CHEMBL614582
IC50 8.72 8.72 1.9 1
SW480
CHEMBL612544
IC50 8.7 8.7 2.0 1
WiDr
CHEMBL614647
IC50 8.68 8.68 2.1 1
HT-29
CHEMBL384
IC50 8.64 8.64 2.3 1
Dihydrofolate reductase
CHEMBL202
IC50 8.42 8.42 3.8 2
Thymidylate synthase
CHEMBL3160
IC50 6.72 6.72 190.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
2738891 10.1021/jm00127a026 Sus scrofa 2
110930 10.1021/jm00191a005 Dihydrofolate reductase 2
2738891 10.1021/jm00127a026 Dihydrofolate reductase 1
3339615 10.1021/jm00397a031 Thymidylate synthase 1
3339615 10.1021/jm00397a031 Dihydrofolate reductase 1
3612694 10.1021/jm00391a042 HuTu80 1
3612694 10.1021/jm00391a042 HT-29 1
3612694 10.1021/jm00391a042 SW480 1
3612694 10.1021/jm00391a042 WiDr 1

Data from ChEMBL 36 via Core Engine