General Information
ZINC ID ZINC000001553379
Molecular Weight (Da)367
SMILESCCCCn1c2c(cc(C(=O)NCc3ccccc3)c1=O)CCCCCC2
Molecular FormulaC23N2O2
ActionAgonist
Chemical Structure
Physicochemical Details
Molar Refractivity109.213
HBA2
HBD1
Rotatable Bonds6
Heavy Atoms27
LogP5.423
Activity (Ki) in nM1.413
Polar Surface Area (PSA)51.1
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 binding1.02354157
Chemical Structure
Pharmacokinetic Properties (SwissADME)
Number of aromatic heavy atoms12
Fraction csp30.48
Ilogp3.47
Xlogp35.01
Wlogp4.09
Mlogp3.72
Silicos-it log p5.06
Consensus log p4.27
Esol log s-5.14
Esol solubility (mg/ml)0.00268
Esol solubility (mol/l)0.00000732
Esol classModerately
Ali log s-5.82
Ali solubility (mg/ml)0.000551
Ali solubility (mol/l)0.0000015
Ali classModerately
Silicos-it logsw-7.25
Silicos-it solubility (mg/ml)0.0000208
Silicos-it solubility (mol/l)5.68E-08
Silicos-it classPoorly soluble
Pgp substrate
Log kp (cm/s)-4.98
Lipinski number of violations0
Ghose number of violations0
Veber number of violations0
Egan number of violations0
Muegge number of violations1
Bioavailability score0.55
Pains number of alerts0
Brenk number of alerts0
Leadlikeness number of violations2
Synthetic accessibility3.26
Chemical Structure
Pharmacokinetic Properties (ADMETLab)
Logs-5.724
Logd4.078
Logp5.259
F (20%)0.716
F (30%)0.998
Mdck1.75E-05
Ppb0.9737
Vdss2.209
Fu0.0083
Cyp1a2-inh0.623
Cyp1a2-sub0.463
Cyp2c19-inh0.863
Cyp2c19-sub0.083
Cl4.562
T120.145
H-ht0.812
Dili0.266
Roa0.644
Fdamdd0.336
Skinsen0.397
Ec0.003
Ei0.014
Respiratory0.064
Bcf1.245
Igc505.062
Lc505.552
Lc50dm5.527
Nr-ar0.059
Nr-ar-lbd0.004
Nr-ahr0.628
Nr-aromatase0.543
Nr-er0.24
Nr-er-lbd0.009
Nr-ppar-gamma0.59
Sr-are0.309
Sr-atad50.017
Sr-hse0.113
Sr-mmp0.497
Sr-p530.079
Vol401.814
Dense0.911
Flex0.333
Nstereo0
Nongenotoxic carcinogenicity0
Ld50 oral0
Genotoxic carcinogenicity mutagenicity0
Surechembl0
Nonbiodegradable1
Skin sensitization1
Acute aquatic toxicity0
Toxicophores0
Qed0.831
Synth2.163
Fsp30.478
Mce-1837.647
Natural product-likeness-1.177
Alarm nmr0
Bms0
Chelating0
Pfizer0
GskRejected
GoldentriangleAccepted