General Information
ZINC ID ZINC000028962232
Molecular Weight (Da)357
SMILESO=c1c2cn(Cc3ccccc3)c3ccccc3c-2nn1C1CCCCC1
Molecular FormulaC23N3O1
ActionAgonist
Chemical Structure
Physicochemical Details
Molar Refractivity107.627
HBA2
HBD0
Rotatable Bonds3
Heavy Atoms27
LogP5.165
Activity (Ki) in nM616.595
Polar Surface Area (PSA)39.82
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 binding1.18888485
Chemical Structure
Pharmacokinetic Properties (SwissADME)
Number of aromatic heavy atoms19
Fraction csp30.3
Ilogp3.76
Xlogp34.71
Wlogp4.9
Mlogp4.41
Silicos-it log p4.02
Consensus log p4.36
Esol log s-5.35
Esol solubility (mg/ml)0.00161
Esol solubility (mol/l)0.00000451
Esol classModerately
Ali log s-5.27
Ali solubility (mg/ml)0.0019
Ali solubility (mol/l)0.00000531
Ali classModerately
Silicos-it logsw-6.78
Silicos-it solubility (mg/ml)0.0000588
Silicos-it solubility (mol/l)0.00000016
Silicos-it classPoorly soluble
Pgp substrate
Log kp (cm/s)-5.14
Lipinski number of violations1
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 violations2
Synthetic accessibility2.74
Chemical Structure
Pharmacokinetic Properties (ADMETLab)
Logs-6.586
Logd4.286
Logp4.901
F (20%)0.79
F (30%)0.003
Mdck-
Ppb97.49%
Vdss1.67
Fu0.95%
Cyp1a2-inh0.744
Cyp1a2-sub0.448
Cyp2c19-inh0.889
Cyp2c19-sub0.07
Cl9.472
T120.021
H-ht0.347
Dili0.845
Roa0.075
Fdamdd0.392
Skinsen0.213
Ec0.003
Ei0.036
Respiratory0.794
Bcf2.249
Igc504.907
Lc505.896
Lc50dm5.61
Nr-ar0.055
Nr-ar-lbd0.009
Nr-ahr0.546
Nr-aromatase0.86
Nr-er0.57
Nr-er-lbd0.024
Nr-ppar-gamma0.105
Sr-are0.806
Sr-atad50.307
Sr-hse0.496
Sr-mmp0.654
Sr-p530.747
Vol381.634
Dense0.936
Flex0.107
Nstereo0
Nongenotoxic carcinogenicity1
Ld50 oral0
Genotoxic carcinogenicity mutagenicity3
Surechembl0
Nonbiodegradable1
Skin sensitization0
Acute aquatic toxicity-
Toxicophores1
Qed0.525
Synth2.242
Fsp30.304
Mce-1857.6
Natural product-likeness-1.112
Alarm nmr0
Bms0
Chelating0
Pfizer-
GskRejected
GoldentriangleAccepted