Detailed Information for D01413

Basic information about inhibitors

IPAD-DB ID D01413
Name Raltitrexed
Category Drugs
2D Structure
3D Structure
Molecular Formula C 2 1 H 2 2 N 4 O 6 S
Molecular Weight 458.5 g/mol
IUPAC Name (2S)-2-[[5-[methyl-[(2-methyl-4-oxo-3H-quinazolin-6-yl)methyl]amino]thiophene-2-carbonyl]amino]pentanedioic acid
InChI InChI=1S/C21H22N4O6S/c1-11-22-14-4-3-12(9-13(14)19(28)23-11)10-25(2)17-7-6-16(32-17)20(29)24-15(21(30)31)5-8-18(26)27/h3-4,6-7,9,15H,5,8,10H2,1-2H3,(H,24,29)(H,26,27)(H,30,31)(H,22,23,28)/t15-/m0/s1
InChIKey IVTVGDXNLFLDRM-HNNXBMFYSA-N
Canonical SMILES CC1=NC2=C(C=C(C=C2)CN(C)C3=CC=C(S3)C(=O)NC(CCC(=O)O)C(=O)O)C(=O)N1
PubChem CID 135400182
DrugBank Accession Number DB00293
CAS Registry Number 112887-68-0

Biological activity data

Ki
EC50
IC50
Inhibition
Toxicity
ROS(reactive oxygen species) -
Metal Chelating -
BBB(blood-brain barrier) -
Target Protein Aβ42
Effects
Research Models Molecular docking
Ref. Link

Physicochemical properties

Molecular Weight(Computed by SwissADME) 458.49
Hac(Computed by SwissADME) 32
Volume(Computed by ADMETlab 2.0) 434.976
Density(Computed by ADMETlab 2.0) 1.053
nRing(Computed by ADMETlab 2.0) 3
MaxRing(Computed by ADMETlab 2.0) 3
nHet(Computed by ADMETlab 2.0) 11
fChar(Computed by ADMETlab 2.0) 0
nRig(Computed by ADMETlab 2.0) 20
Flexibility(Computed by ADMETlab 2.0) 0.5
Stero Centers(Computed by ADMETlab 2.0) 1
LogS(Computed by ADMETlab 2.0) -5.178
LogD(Computed by ADMETlab 2.0) 0.336

ADMET properties

logP(Computed by ADMETlab 2.0) 0.651
TPSA(Computed by SwissADME) 180.93
Hbond Acceptor(Computed by SwissADME) 7
Hbond Donor(Computed by SwissADME) 4
Rotatable Bonds(Computed by SwissADME) 10

Pharmacokinetics

GI Absorption(Computed by SwissADME) Low
BBB(blood-brain barrier) Permeant(Computed by SwissADME) No
P-gp Substrate(Computed by SwissADME) Yes
CYP1A2 Inhibitor(Computed by SwissADME) No
CYP2C19 Inhibitor(Computed by SwissADME) No
CYP2C9 Inhibitor(Computed by SwissADME) No
CYP2D6 Inhibitor(Computed by SwissADME) No
CYP3A4 Inhibitor(Computed by SwissADME) No
log Kp(Skin Permeation)(Computed by SwissADME) -8.09

Druglikeness

Lipinski(Computed by SwissADME) 0
Ghose(Computed by SwissADME) 0
Veber(Computed by SwissADME) 1
Egan(Computed by SwissADME) 1
Muegge(Computed by SwissADME) 1
Bioavailability Score(Computed by SwissADME) 0.11