Assay ID | Title | Year | Journal | Article |
AID552178 | Inhibition of [3H]E1 binding to human placental 17beta-HSD1 after 20 mins | 2011 | Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2
| 17β-HSD2 inhibitors for the treatment of osteoporosis: Identification of a promising scaffold. |
AID366235 | Terminal half life in Wistar rat at 10 mg/kg, po | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokinetics. |
AID318313 | Inhibition of human CYP2C9 | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent disease |
AID366227 | Displacement of [3H]17beta-estradiol from human recombinant ERalpha receptor relative to estradiol | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokinetics. |
AID242151 | Inhibition of [3H]17-beta-estradiol binding to human estrogen receptor alpha expressed in Escherichia coli | 2005 | Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12
| ERbeta ligands. 3. Exploiting two binding orientations of the 2-phenylnaphthalene scaffold to achieve ERbeta selectivity. |
AID552174 | Inhibition of [3H]E2 binding to human placental 17beta-HSD2 at 1 uM after 20 mins | 2011 | Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2
| 17β-HSD2 inhibitors for the treatment of osteoporosis: Identification of a promising scaffold. |
AID318307 | Displacement of [3H]estradiol from human recombinant ERbeta relative to estradiol | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent disease |
AID318312 | Inhibition of human CYP2B6 | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent disease |
AID566782 | Displacement of [3H]E2 from human recombinant ERbeta by liquid scintillation counting relative to estradiol | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| New drug-like hydroxyphenylnaphthol steroidomimetics as potent and selective 17β-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of estrogen-dependent diseases. |
AID318306 | Displacement of [3H]estradiol from human recombinant ERalpha relative to estradiol | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent disease |
AID566723 | Selectivity ratio of IC50 for human placental 17beta-HSD2 to IC50 for human placental 17beta-HSD1 | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| New drug-like hydroxyphenylnaphthol steroidomimetics as potent and selective 17β-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of estrogen-dependent diseases. |
AID366219 | Inhibition of human recombinant 17beta-HSD1 expressed in Sf9 cells assessed as conversion of [3H]estrone to [3H]17beta-estradiol at 1 uM | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokinetics. |
AID242135 | Inhibition of [3H]17-beta-estradiol binding to human estrogen receptor beta expressed in Escherichia coli | 2005 | Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12
| ERbeta ligands. 3. Exploiting two binding orientations of the 2-phenylnaphthalene scaffold to achieve ERbeta selectivity. |
AID318315 | Inhibition of human CYP2D6 | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent disease |
AID366236 | AUC (0 to tlast) in Wistar rat at 10 mg/kg, po | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokinetics. |
AID318304 | Inhibition of human placental 17beta-HSD2 | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent disease |
AID552180 | Displacement of [3H]E2 from human recombinant ERalpha by liquid scintillation counting relative to estradiol | 2011 | Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2
| 17β-HSD2 inhibitors for the treatment of osteoporosis: Identification of a promising scaffold. |
AID318309 | Metabolic stability assessed as half life in rat liver microsomes | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent disease |
AID566781 | Displacement of [3H]E2 from human recombinant ERalpha by liquid scintillation counting relative to estradiol | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| New drug-like hydroxyphenylnaphthol steroidomimetics as potent and selective 17β-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of estrogen-dependent diseases. |
AID318303 | Inhibition of human placental 17beta-HSD1 | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent disease |
AID552177 | Inhibition of [3H]E2 binding to human placental 17beta-HSD2 after 20 mins | 2011 | Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2
| 17β-HSD2 inhibitors for the treatment of osteoporosis: Identification of a promising scaffold. |
AID305160 | Inhibition of mushroom tyrosinase | 2007 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
| Syntheses of hydroxy substituted 2-phenyl-naphthalenes as inhibitors of tyrosinase. |
AID243121 | Relative inhibition of [3H]17-beta-estradiol binding to human estrogen receptor alpha and beta expressed in Escherichia coli | 2005 | Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12
| ERbeta ligands. 3. Exploiting two binding orientations of the 2-phenylnaphthalene scaffold to achieve ERbeta selectivity. |
AID366225 | Inhibition of human placental 17beta-HSD2 assessed as conversion of [3H]17beta-estradiol to [3H]estrone | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokinetics. |
AID318301 | Inhibition of human recombinant 17beta-HSD1 expressed in Sf9 insect cells at 100 nM | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent disease |
AID366230 | Stimulation of human T47C cell proliferation at 100 nM after 8 days by MTT assay relative to 17-beta estradiol | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokinetics. |
AID552181 | Displacement of [3H]E2 from human recombinant ERbeta by liquid scintillation counting relative to estradiol | 2011 | Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2
| 17β-HSD2 inhibitors for the treatment of osteoporosis: Identification of a promising scaffold. |
AID566722 | Displacement of [3H]E1 from human placental 17beta-HSD1 after 10 mins by fluid scintillation counting | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| New drug-like hydroxyphenylnaphthol steroidomimetics as potent and selective 17β-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of estrogen-dependent diseases. |
AID366226 | Selectivity ratio, IC50 for human placental 17beta-HSD2 to IC50 for human placental 17beta-HSD1 | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokinetics. |
AID366237 | AUC (0 to infinity) in Wistar rat at 10 mg/kg, po | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokinetics. |
AID318311 | Inhibition of human CYP1A2 | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent disease |
AID366228 | Displacement of [3H]17beta-estradiol from human recombinant ERbeta receptor relative to estradiol | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokinetics. |
AID366233 | Tmax in Wistar rat at 10 mg/kg, po | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokinetics. |
AID318314 | Inhibition of human CYP2C19 | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent disease |
AID366234 | Tlast in Wistar rat at 10 mg/kg, po | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokinetics. |
AID566780 | Displacement of [3H]E1 from 17beta-HSD1 in human T47D cells after 10 mins by fluid scintillation counting | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| New drug-like hydroxyphenylnaphthol steroidomimetics as potent and selective 17β-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of estrogen-dependent diseases. |
AID366222 | Inhibition of human placental 17beta-HSD2 assessed as conversion of [3H]17beta-estradiol to [3H]estrone at 1 uM | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokinetics. |
AID318310 | Metabolic stability assessed as intrinsic body clearance in rat liver microsomes | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent disease |
AID318308 | Apparent permeability across human Caco-2 cell membrane | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent disease |
AID366232 | Clast in Wistar rat at 10 mg/kg, po | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokinetics. |
AID566721 | Displacement of [3H]E2 from human placental 17beta-HSD2 after 10 mins by fluid scintillation counting | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| New drug-like hydroxyphenylnaphthol steroidomimetics as potent and selective 17β-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of estrogen-dependent diseases. |
AID366218 | Inhibition of human recombinant 17beta-HSD1 expressed in Sf9 cells assessed as conversion of [3H]estrone to [3H]17beta-estradiol at 100 nM | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokinetics. |
AID552175 | Inhibition of [3H]E1 binding to human placental 17beta-HSD1 at 1 uM after 20 mins | 2011 | Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2
| 17β-HSD2 inhibitors for the treatment of osteoporosis: Identification of a promising scaffold. |
AID318302 | Inhibition of human recombinant 17beta-HSD1 expressed in Sf9 insect cells at 1 uM | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent disease |
AID366231 | Cmax in Wistar rat at 10 mg/kg, po | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokinetics. |
AID366224 | Inhibition of human placental 17beta-HSD1 assessed as conversion of [3H]estrone to [3H]17beta-estradiol | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokinetics. |
AID552179 | Selectivity ratio of IC50 for human placental 17beta-HSD1 to IC50 for human placental 17beta-HSD2 | 2011 | Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2
| 17β-HSD2 inhibitors for the treatment of osteoporosis: Identification of a promising scaffold. |
AID318305 | Selectivity ratio for human placental 17beta-HSD1 over human placental 17beta-HSD2 | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent disease |
AID318316 | Inhibition of human CYP3A4 | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent disease |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |