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Compound Detail

CHEMBL296373

EDATREXATE
🧪 Phase II
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🧪 Phase II
CCC(Cc1cnc2nc(N)nc(N)c2n1)c1ccc(C(=O)N[C@@H](CCC(=O)O)C(=O)O)cc1

Basic Information

ChEMBL ID CHEMBL296373
Name EDATREXATE
Phase Phase II
Structure Type MOL
InChI Key FSIRXIHZBIXHKT-MHTVFEQDSA-N

Known Names

CGP 30694 CGP-30694 Edatrexate Edatrexato GNF-PF-63 NSC-626715 TCMDC-137768
12
Targets
37
Activities
3
Assay Types
0
PK Parameters
20
Publications
7
Known Names

Molecular Properties

467.5
MW (Da)
1.37
ALogP
9
HBA
5
HBD
207.3
PSA (Ų)
0.29
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Racemic

Flags

Natural Product
USAN Stem -trexate
USAN Year 1990

Extended Properties

Molecular Formula C22H25N7O5
MW 467.49
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.12

Activity Summary

IC50 31 meas. best 9.8
Ki 4 meas. best 6.08
EC50 2 meas. best 7.83

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Lacticaseibacillus casei
CHEMBL613075
IC50 9.8 7.4629 0.2 14
L1210
CHEMBL386
IC50 9.19 9.19 0.7 1
Mus musculus
CHEMBL375
IC50 8.84 8.84 1.4 1
Dihydrofolate reductase
CHEMBL202
IC50 8.59 8.475 2.6 2
KB
CHEMBL398
IC50 8.52 8.52 3.0 1
CCRF-CEM
CHEMBL382
IC50 8.48 8.48 3.3 1
Dihydrofolate reductase
CHEMBL2902
IC50 8.42 7.865 3.8 6
P388
CHEMBL389
IC50 8.37 7.865 4.3 2
Colon 26
CHEMBL614466
IC50 8.32 8.32 4.8 1
Dihydrofolate reductase
CHEMBL4564
IC50 7.96 7.96 11.0 1
MC-38
CHEMBL612821
IC50 7.96 7.96 11.0 1
Plasmodium falciparum
CHEMBL364
EC50 7.83 7.4 14.8 2
Mus musculus
CHEMBL375
Ki 6.08 6.08 830.0 1
Dihydrofolate reductase
CHEMBL4564
Ki 6.0 6.0 990.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Lacticaseibacillus casei IC50 = 0.16 nM 9.8 Inhibitory activity against the growth of Lactobacillus casei (ATCC 7469) was de... 2447278
Lacticaseibacillus casei IC50 = 0.63 nM 9.2 Inhibitory activity against the growth of Lactobacillus casei (ATCC 7469) was de... 2447278
L1210 IC50 = 0.65 nM 9.19 Concentration inhibiting L1210 cell growth in culture 2296020
Lacticaseibacillus casei IC50 = 1.0 nM 9.0 Inhibitory activity against the growth of Lactobacillus casei (ATCC 7469) was de... 2447278
Mus musculus IC50 = 1.44 nM 8.84 Inhibition of growth in L1210 murine leukemia cells in culture expressed as IC50... 8340923
Dihydrofolate reductase IC50 = 2.6 nM 8.59 Tested in vitro for inhibitory concentration against CCRF-CEM human Leukemic lym... 8035423
KB IC50 = 3.0 nM 8.52 Inhibitory concentration of compound was tested against KB tumor growth cell lin... 8201595
CCRF-CEM IC50 = 3.3 nM 8.48 Growth inhibition of CCRF-CEM human leukemic lymphoblasts 10780919
Dihydrofolate reductase IC50 = 3.8 nM 8.42 Compound was tested for the inhibition of dihydrofolate reductase in Bovine live... 8201595
P388 IC50 = 4.3 nM 8.37 Inhibitory concentration of compound was tested against P388 tumor growth cell l... 8201595
Dihydrofolate reductase IC50 = 4.4 nM 8.36 Compound was tested for its inhibitory activity on Recombinant Human Dihydrofola... 1992121
Colon 26 IC50 = 4.8 nM 8.32 Inhibitory concentration of compound was tested against Colon 26 tumor growth ce... 8201595
Lacticaseibacillus casei IC50 = 7.0 nM 8.15 Inhibitory activity against the growth of Streptococcus faecium (ATCC 8043) was ... 2447278
Lacticaseibacillus casei IC50 = 7.4 nM 8.13 Inhibitory activity against thymidylate synthase in Lactobacillus casei was dete... 2447278
Dihydrofolate reductase IC50 = 9.0 nM 8.05 Inhibitory activity against dihydrofolate reductase in Lactobacillus casei was d... 2447278
Dihydrofolate reductase IC50 = 9.0 nM 8.05 Inhibitory activity against dihydrofolate reductase in Lactobacillus casei was d... 2447278
Lacticaseibacillus casei IC50 = 9.0 nM 8.05 Inhibitory activity against the growth of Lactobacillus casei (ATCC 7469) was de... 2447278
Dihydrofolate reductase IC50 = 11.0 nM 7.96 Compound was tested for the inhibition of dihydrofolate reductase in P388 cells 8201595
MC-38 IC50 = 11.0 nM 7.96 Inhibitory concentration of compound was tested against Colon 38 tumor growth ce... 8201595
Lacticaseibacillus casei IC50 = 14.0 nM 7.85 Inhibitory activity against thymidylate synthase in Lactobacillus casei was dete... 2447278

Literature References

PubMed DOI Target Context # Activities
2447278 10.1021/jm00396a029 Lacticaseibacillus casei 18
9022804 10.1021/jm9505526 Mus musculus 16
8201595 10.1021/jm00037a012 Mus musculus 14
15646539 10.1016/s0399-8320(04)95062-2 Unchecked 11
15646539 10.1016/s0399-8320(04)95062-2 NON-PROTEIN TARGET 8
2447278 10.1021/jm00396a029 Dihydrofolate reductase 6
20485427 10.1038/nature09107 Plasmodium falciparum 4
18579783 10.1073/pnas.0802982105 Plasmodium falciparum 2
8035423 10.1021/jm00040a008 Dihydrofolate reductase 2
- 10.1016/0960-894X(96)00053-4 Folylpolyglutamate synthase, mitochondrial 2
8340923 10.1021/jm00067a020 Mus musculus 2
2296020 10.1021/jm00163a035 Dihydrofolate reductase 2
8201595 10.1021/jm00037a012 Colon 26 2
8201595 10.1021/jm00037a012 P388 2
8201595 10.1021/jm00037a012 Dihydrofolate reductase 2
10780919 10.1021/jm990630f CCRF-CEM 1
8340923 10.1021/jm00067a020 Dihydrofolate reductase 1
2296020 10.1021/jm00163a035 L1210 1
8201595 10.1021/jm00037a012 MC-38 1
- 10.6019/CHEMBL3433997 Glucose transporter 1

Data from ChEMBL 36 via Core Engine