General Information
ZINC ID ZINC000147446839
Molecular Weight (Da)321
SMILESCC(C)(C)c1cc(NC(=O)[C@@H]2CCCN2C2CCOCC2)on1
Molecular FormulaC17N3O3
ActionAgonist
Chemical Structure
Physicochemical Details
Molar Refractivity86.095
HBA4
HBD1
Rotatable Bonds4
Heavy Atoms23
LogP2.037
Activity (Ki) in nM2.818
Polar Surface Area (PSA)67.6
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
-
Biodegradation0
Glucocorticoid receptor binding+
Thyroid receptor binding-
Androgen receptor binding-
Plasma protein binding0.74224698
Chemical Structure
Pharmacokinetic Properties (SwissADME)
Number of aromatic heavy atoms5
Fraction csp30.76
Ilogp3.1
Xlogp32.58
Wlogp1.98
Mlogp1.1
Silicos-it log p2.14
Consensus log p2.18
Esol log s-3.29
Esol solubility (mg/ml)0.165
Esol solubility (mol/l)0.000514
Esol classSoluble
Ali log s-3.65
Ali solubility (mg/ml)0.0723
Ali solubility (mol/l)0.000225
Ali classSoluble
Silicos-it logsw-3.54
Silicos-it solubility (mg/ml)0.0925
Silicos-it solubility (mol/l)0.000288
Silicos-it classSoluble
Pgp substrate
Log kp (cm/s)-6.43
Lipinski number of violations0
Ghose number of violations0
Veber number of violations0
Egan number of violations0
Muegge number of violations0
Bioavailability score0.55
Pains number of alerts0
Brenk number of alerts0
Leadlikeness number of violations0
Synthetic accessibility3.97
Chemical Structure
Pharmacokinetic Properties (ADMETLab)
Logs-1.467
Logd2.223
Logp2.201
F (20%)0.003
F (30%)0.005
Mdck1.08E-05
Ppb0.6282
Vdss1.011
Fu0.4423
Cyp1a2-inh0.041
Cyp1a2-sub0.138
Cyp2c19-inh0.111
Cyp2c19-sub0.469
Cl5.646
T120.809
H-ht0.95
Dili0.655
Roa0.914
Fdamdd0.897
Skinsen0.13
Ec0.003
Ei0.012
Respiratory0.939
Bcf1.033
Igc502.351
Lc503.456
Lc50dm4.507
Nr-ar0.004
Nr-ar-lbd0.002
Nr-ahr0.011
Nr-aromatase0.006
Nr-er0.218
Nr-er-lbd0.008
Nr-ppar-gamma0.004
Sr-are0.247
Sr-atad50.002
Sr-hse0.005
Sr-mmp0.053
Sr-p530.013
Vol328.37
Dense0.978
Flex0.222
Nstereo1
Nongenotoxic carcinogenicity0
Ld50 oral0
Genotoxic carcinogenicity mutagenicity0
Surechembl0
Nonbiodegradable2
Skin sensitization0
Acute aquatic toxicity0
Toxicophores0
Qed0.904
Synth3.898
Fsp30.765
Mce-1864.8
Natural product-likeness-0.704
Alarm nmr2
Bms0
Chelating0
Pfizer0
GskAccepted
GoldentriangleAccepted