General Information
ZINC ID ZINC000028571872
Molecular Weight (Da)348
SMILESCCc1ccc(-c2cc(O)c3c(c2)OC(C)(C)[C@@H]2CC=C(C)C[C@@H]32)cc1
Molecular FormulaC24O2
ActionPartial Agonist
Chemical Structure
Physicochemical Details
Molar Refractivity107.779
HBA2
HBD1
Rotatable Bonds2
Heavy Atoms26
LogP6.234
Activity (Ki) in nM51.286
Polar Surface Area (PSA)29.46
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 binding0.83969187
Chemical Structure
Pharmacokinetic Properties (SwissADME)
Number of aromatic heavy atoms12
Fraction csp30.42
Ilogp3.9
Xlogp37.41
Wlogp6.23
Mlogp4.79
Silicos-it log p5.87
Consensus log p5.64
Esol log s-6.88
Esol solubility (mg/ml)0.0000461
Esol solubility (mol/l)0.00000013
Esol classPoorly sol
Ali log s-7.86
Ali solubility (mg/ml)0.00000482
Ali solubility (mol/l)1.38E-08
Ali classPoorly sol
Silicos-it logsw-7.21
Silicos-it solubility (mg/ml)0.0000214
Silicos-it solubility (mol/l)6.14E-08
Silicos-it classPoorly soluble
Pgp substrate
Log kp (cm/s)-3.16
Lipinski number of violations1
Ghose number of violations1
Veber number of violations0
Egan number of violations1
Muegge number of violations1
Bioavailability score0.55
Pains number of alerts0
Brenk number of alerts1
Leadlikeness number of violations1
Synthetic accessibility4.28
Chemical Structure
Pharmacokinetic Properties (ADMETLab)
Logs-3.197
Logd5.252
Logp7.827
F (20%)0.956
F (30%)0.966
Mdck1.47E-05
Ppb1.005
Vdss2.811
Fu0.0158
Cyp1a2-inh0.487
Cyp1a2-sub0.733
Cyp2c19-inh0.871
Cyp2c19-sub0.144
Cl5.097
T120.081
H-ht0.954
Dili0.551
Roa0.138
Fdamdd0.941
Skinsen0.341
Ec0.003
Ei0.117
Respiratory0.336
Bcf3.136
Igc505.132
Lc506.492
Lc50dm6.509
Nr-ar0.139
Nr-ar-lbd0.011
Nr-ahr0.629
Nr-aromatase0.834
Nr-er0.513
Nr-er-lbd0.854
Nr-ppar-gamma0.741
Sr-are0.7
Sr-atad50.028
Sr-hse0.524
Sr-mmp0.956
Sr-p530.685
Vol388.56
Dense0.896
Flex0.091
Nstereo2
Nongenotoxic carcinogenicity0
Ld50 oral0
Genotoxic carcinogenicity mutagenicity0
Surechembl0
Nonbiodegradable0
Skin sensitization1
Acute aquatic toxicity0
Toxicophores1
Qed0.652
Synth3.315
Fsp30.417
Mce-1879.059
Natural product-likeness1.562
Alarm nmr0
Bms0
Chelating0
Pfizer0
GskRejected
GoldentriangleRejected