General Information
ZINC ID ZINC000036294632
Molecular Weight (Da)418
SMILESCCCCCn1cc(C(=O)c2cccc3ccccc23)cc1-c1ccc2ccccc2c1
Molecular FormulaC30N1O1
ActionAgonist
Chemical Structure
Physicochemical Details
Molar Refractivity130.558
HBA1
HBD0
Rotatable Bonds7
Heavy Atoms32
LogP7.718
Activity (Ki) in nM169.824
Polar Surface Area (PSA)22
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 binding1.23629534
Chemical Structure
Pharmacokinetic Properties (SwissADME)
Number of aromatic heavy atoms25
Fraction csp30.17
Ilogp4.58
Xlogp37.89
Wlogp7.88
Mlogp4.91
Silicos-it log p7.6
Consensus log p6.57
Esol log s-7.52
Esol solubility (mg/ml)0.0000127
Esol solubility (mol/l)3.05E-08
Esol classPoorly sol
Ali log s-8.2
Ali solubility (mg/ml)0.00000263
Ali solubility (mol/l)6.30E-09
Ali classPoorly sol
Silicos-it logsw-11.03
Silicos-it solubility (mg/ml)3.91E-09
Silicos-it solubility (mol/l)9.38E-12
Silicos-it classInsoluble
Pgp substrate
Log kp (cm/s)-3.25
Lipinski number of violations1
Ghose number of violations2
Veber number of violations0
Egan number of violations1
Muegge number of violations1
Bioavailability score0.55
Pains number of alerts0
Brenk number of alerts0
Leadlikeness number of violations2
Synthetic accessibility3.31
Chemical Structure
Pharmacokinetic Properties (ADMETLab)
Logs-7.302
Logd5.439
Logp7.645
F (20%)0.925
F (30%)0.964
Mdck7.81E-06
Ppb1.0078
Vdss1.046
Fu0.0035
Cyp1a2-inh0.606
Cyp1a2-sub0.175
Cyp2c19-inh0.402
Cyp2c19-sub0.053
Cl4.351
T120.021
H-ht0.08
Dili0.938
Roa0.26
Fdamdd0.428
Skinsen0.688
Ec0.003
Ei0.816
Respiratory0.156
Bcf2.227
Igc505.714
Lc506.335
Lc50dm6.445
Nr-ar0.062
Nr-ar-lbd0.017
Nr-ahr0.679
Nr-aromatase0.917
Nr-er0.914
Nr-er-lbd0.806
Nr-ppar-gamma0.012
Sr-are0.907
Sr-atad50.745
Sr-hse0.13
Sr-mmp0.873
Sr-p530.436
Vol470.167
Dense0.887
Flex0.25
Nstereo0
Nongenotoxic carcinogenicity1
Ld50 oral0
Genotoxic carcinogenicity mutagenicity4
Surechembl0
Nonbiodegradable0
Skin sensitization1
Acute aquatic toxicity0
Toxicophores2
Qed0.195
Synth2.271
Fsp30.167
Mce-1825
Natural product-likeness-0.584
Alarm nmr0
Bms0
Chelating0
Pfizer0
GskRejected
GoldentriangleRejected