General Information
ZINC ID ZINC000299841226
Molecular Weight (Da)357
SMILESCC1CCC(NC(=O)c2cc3cccnc3n(CCC(=O)O)c2=O)CC1
Molecular FormulaC19N3O4
ActionAgonist
Chemical Structure
Physicochemical Details
Molar Refractivity96.101
HBA3
HBD1
Rotatable Bonds5
Heavy Atoms26
LogP2.539
Activity (Ki) in nM1380.384
Polar Surface Area (PSA)101.29
Chemical Structure
Pharmacokinetic Properties (AdmetSAR)
Human intestinal absorption+
Caco-2-
Blood brain barrier-
P-glycoprotein inhibitior-
P-glycoprotein substrate+
Cyp3a4 substrate+
Cyp2c9 substrate-
Cyp2d6 substrate-
Cyp3a4 inhibition-
Cyp2c9 inhibition-
Cyp2c19 inhibition-
Cyp2d6 inhibition-
Cyp1a2 inhibition-
Acute oral toxicity-
Carcinogenicity (binary)-
Ames mutagenesis-
Human ether-a-go-go-related
gene inhibition
-
Biodegradation
Glucocorticoid receptor binding-
Thyroid receptor binding-
Androgen receptor binding-
Plasma protein binding0.82616579
Chemical Structure
Pharmacokinetic Properties (SwissADME)
Number of aromatic heavy atoms10
Fraction csp30.47
Ilogp2.62
Xlogp31.83
Wlogp2.18
Mlogp2.11
Silicos-it log p2.02
Consensus log p2.15
Esol log s-3.1
Esol solubility (mg/ml)2.86E-01
Esol solubility (mol/l)7.99E-04
Esol classSoluble
Ali log s-3.58
Ali solubility (mg/ml)9.46E-02
Ali solubility (mol/l)2.65E-04
Ali classSoluble
Silicos-it logsw-4.14
Silicos-it solubility (mg/ml)2.57E-02
Silicos-it solubility (mol/l)7.19E-05
Silicos-it classModerately soluble
Pgp substrate
Log kp (cm/s)-7.18
Lipinski number of violations0
Ghose number of violations0
Veber number of violations0
Egan number of violations0
Muegge number of violations0
Bioavailability score0.56
Pains number of alerts0
Brenk number of alerts0
Leadlikeness number of violations1
Synthetic accessibility3.44
Chemical Structure
Pharmacokinetic Properties (ADMETLab)
Logs-4.034
Logd0.977
Logp2.023
F (20%)0.005
F (30%)0.474
Mdck5.57E-06
Ppb0.5927
Vdss0.455
Fu0.2323
Cyp1a2-inh0.134
Cyp1a2-sub0.055
Cyp2c19-inh0.193
Cyp2c19-sub0.061
Cl2.016
T120.552
H-ht0.77
Dili0.865
Roa0.34
Fdamdd0.5
Skinsen0.157
Ec0.003
Ei0.017
Respiratory0.049
Bcf0.416
Igc502.789
Lc503.573
Lc50dm3.871
Nr-ar0.558
Nr-ar-lbd0.005
Nr-ahr0.054
Nr-aromatase0.013
Nr-er0.213
Nr-er-lbd0.085
Nr-ppar-gamma0.672
Sr-are0.298
Sr-atad50.013
Sr-hse0.032
Sr-mmp0.037
Sr-p530.046
Vol361.207
Dense0.989
Flex20
Nstereo0.3
Nongenotoxic carcinogenicity0
Ld50 oral0
Genotoxic carcinogenicity mutagenicity0
Surechembl0
Nonbiodegradable0
Skin sensitization1
Acute aquatic toxicity0
Toxicophores0
Qed0
Synth0.854
Fsp32.342
Mce-180.474
Natural product-likeness43.714
Alarm nmr-1.128
Bms0
Chelating0
Pfizer0
GskAccepted
GoldentriangleAccepted