Target Poor or Non Binder(s) Information

Target General Information

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Target ID

T22939

Target Info

Target Name

Progesterone receptor (PGR)

Synonyms

PR; Nuclear receptor subfamily 3 group C member 3; NR3C3

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Target Type

Successful Target

Gene Name

PGR

Biochemical Class

Nuclear hormone receptor

UniProt ID

P06401

Poor Binders of This Target (in total, 13 binders)

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Compound Name

Tamoxifen

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Approved

Compound Info

Synonyms

tamoxifen; 10540-29-1; trans-Tamoxifen; Crisafeno; Soltamox; Tamoxifene; Diemon; Tamoxifenum; Tamoxifeno; Tamizam; Istubol; Tamoxen; Citofen; Oncomox; Valodex; Retaxim; Tamoxifene [INN-French]; Tamoxifenum [INN-Latin]; Tamoxifeno [INN-Spanish]; Tamoxifen (Z); Tamoxifen and its salts; Tamoxifen [INN:BAN]; ICI-46474; ICI 47699; TRANS FORM OF TAMOXIFEN; CCRIS 3275; UNII-094ZI81Y45; HSDB 6782; CHEMBL83; EINECS 234-118-0; 1-p-beta-Dimethylaminoethoxyphenyl-trans-1,2-diphenylbut-1-ene; Citofen; Nourytam; Novaldex; Tamone; Tamoxifeno;Tamoxifenum; Tomaxithen; Gen-Tamoxifen; Istubal (TN); Nolvadex (TN); Nolvadex-D; Novo-Tamoxifen; Pms-Tamoxifen; Tamoplex (TN); Tamoxifen (INN); Tamoxifen (TN); Trans-Tamoxifen; Valodex (TN); TAMOXIFEN (TAMOXIFEN CITRATE (54965-24-1)); Trans-2-[4-(1,2-Diphenyl-1-butenyl)phenoxy]-N,N-dimethylethylamine; (Z)-1-(p-Dimethylaminoethoxyphenyl)-1,2-diphenyl-1-butene; (Z)-2-(4-(1,2-Diphenyl-1-butenyl)phenoxy)-N,N-dimethylethanamine; (Z)-2-(4-(1,2-diphenylbut-1-enyl)phenoxy)-N,N-dimethylethanamine; (Z)-2-(para-(1,2-Diphenyl-1-butenyl)phenoxy)-N,N-dimethylamine (IUPAC); (Z)-2-[4-(1,2)-DIPHENYL-1-BUTENYL)-PHENOXY]-N,N-DIMETHYLETHANAMINE; (Z)-2-[p-(1,2-Diphenyl-1-butenyl)phenoxy]-N,N-dimethylethylamine; 1-p-beta-Dimethylamino-ethoxyphenyl-trans-1,2-diphenylbut-1-ene; 1-para-beta-Dimethylaminoethoxyphenyl-trans-1,2-diphenylbut-1-ene; 2-[4-[(Z)-1,2-diphenylbut-1-enyl]phenoxy]-N,N-dimethylethanamine; 2-{4-[(1Z)-1,2-diphenylbut-1-en-1-yl]phenoxy}-N,N-dimethylethanamine; Tamoxifen (Hormonal therapy); [3H]tamoxifen

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Activity

IC50 ~ 100000 nM

[1]

Compound Name

Fulvestrant

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Approved

Compound Info

Synonyms

Faslodex; AstraZeneca brand of fulvestrant; Fulvestrant [USAN]; Ici 182780; ZD 182780; ZM 182780; Faslodex (TN); ZD-182780; ZD-9238; ZM-182780; Faslodex(ICI 182,780); Faslodex, ICI 182780, Fulvestrant; Fulvestrant (JAN/USAN/INN); (7R,13S,17S)-13-methyl-7-(9-(4,4,5,5,5-pentafluoropentylsulfinyl)nonyl)-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diol; (7R,8R,9S,13S,14S,17S)-13-methyl-7-[9-(4,4,5,5,5-pentafluoropentylsulfinyl)nonyl]-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol; (7R,8S,9S,13S,14S,17S)-13-methyl-7-[9-(4,4,5,5,5-pentafluoropentylsulfinyl) nonyl]-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol; (7alpha,17beta)-7-{9-[(4,4,5,5,5-pentafluoropentyl)sulfinyl]nonyl}estra-1,3,5(10)-triene-3,17-diol; 7-(9-(4,4,5,5,5-pentafluoropentylsulfinyl)nonyl)estra-1,3,5(10)-triene-3,17-diol; 7alpha-(9-((4,4,5,5,5,-Pentafluoropentyl)sulfinyl)nonyl)estra-1,3,5(10)-triene-3,17beta-diol; 7alpha-(9-((4,4,5,5,5-Pentafluoropentyl)sulfinyl)nonyl)estra-1,3,5(10)-triene-3,17beta-diol; 7alpha-[9[(4,4,5,5,5-Pentafluropentyl)sulfinyl]nonyl]-estra-1,3,5(10)-triene-3, 17 beta diol; ICI

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Activity

IC50 ~ 100000 nM

[1]

Compound Name

6-(5-Chlorothiophen-2-yl)chromen-2-one

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Investigative

Compound Info

Synonyms

CHEMBL1835834; BDBM50355241

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Activity

IC50 = 50500 nM

[2]

Compound Name

1-Methyl-3-phenyl-2,4(1H,3H)-quinazolinedione

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Investigative

Compound Info

Synonyms

1-methyl-3-phenylquinazoline-2,4(1H,3H)-dione; 1-methyl-3-phenylquinazoline-2,4-dione; CHEMBL479738; NSC51430; SCHEMBL6360759; CTK0I3962; KCTNJALTDRHVIE-UHFFFAOYSA-; DTXSID80287519; ZINC1682604; BDBM50251662; NSC-51430; STK235534; AKOS002306885; CCG-275582; MCULE-7387273970; 1-methyl-3-phenyl-quinazoline-2,4-dione; ST50760223; 1-methyl-3-phenyl-1,3-dihydroquinazoline-2,4-dione

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Activity

IC50 = 84000 nM

[3]

Compound Name

(E)-3-[4-[(1R,3R)-2-(2-Hydroxyethyl)-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]phenyl]prop-2-enoic acid

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Investigative

Compound Info

Synonyms

CHEMBL3622998; BDBM50125080

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Activity

IC50 ~ 100000 nM

[1]

Compound Name

Afimoxifene

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Investigative

Compound Info

Synonyms

(Z)-4-(1-(4-(2-(Dimethylamino)ethoxy)-phenyl)-2-phenylbut-1-en-1-yl)phenol; (Z)-4-(1-[4-(Dimethylaminoethoxy)phenyl]-2-phenyl-1-butenyl)phenol; (E/Z)-4-Hydroxytamoxifen; 4-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol; DSSTox_CID_28161; DSSTox_RID_79302; DSSTox_GSID_37094; MLS003106263; CHEMBL2137046; DTXSID3037094; BCBcMAP01_000199; CTK8E2879; CTK8E7487; HMS3370G08; BCP04749; BCP23058; Tox21_303657; BDBM50276802; s7827; AKOS028114525; Phenol, 4-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenyl-1-butenyl]-; CCG-268491; 4-Hydroxytamoxifen (4-HT, Afimoxifene; SMP1_000161; NCGC00249622-01; NCGC00257332-01; SMR001819827; FT-0647372; FT-0670138; FT-0670142; FT-0670146; KS-00001838; Q27163871; (E)-4-(1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenol

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Activity

IC50 ~ 100000 nM

[1]

Compound Name

(E)-3-[4-[(1R,3R)-2-[(2R)-3-Hydroxy-2-methylpropyl]-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]phenyl]prop-2-enoic acid

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Investigative

Compound Info

Synonyms

CHEMBL3623000; BDBM50125078

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Activity

IC50 ~ 100000 nM

[1]

Compound Name

2-[1-(4-Chlorophenyl)-1,3,4,9-tetrahydropyrido[3,4-b]indol-2-yl]ethanol

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Investigative

Compound Info

Synonyms

CHEMBL3622992; BDBM50125086

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Activity

IC50 ~ 100000 nM

[1]

Compound Name

3-[(1R,3R)-1-(4-Chlorophenyl)-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-2-yl]propanoic acid

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Investigative

Compound Info

Synonyms

CHEMBL3622995; BDBM50125083; (1R,3R)-1-(4-Chlorophenyl)-3-methyl-1,2,3,4-tetrahydro-beta-carboline-2-propionic acid

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Activity

IC50 ~ 100000 nM

[1]

Compound Name

(E)-3-[4-[(1R,3R)-3-Methyl-2-(2-methylpropyl)-1,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]phenyl]prop-2-enoic acid

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Investigative

Compound Info

Synonyms

CHEMBL3623001; BDBM50125077; (E)-3-(4-((1R,3R)-2-Isobutyl-3-methyl-1,2,3,4-tetrahydro-beta-carboline-1-yl)phenyl)acrylic acid

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Activity

IC50 ~ 100000 nM

[1]

Compound Name

(2E)-3-{4-[(1E)-1,2-Diphenylbut-1-enyl]phenyl}acrylic acid

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Investigative

Compound Info

Synonyms

Etacstil; GW5638; GW 5638; GW-5638; CHEMBL33899; 3-(4-(1,2-Diphenylbut-1-enyl)phenyl)acrylic acid; 4-(1,2-Diphenyl-1-butenyl)cinnamic acid; BIDD:ER0054; SCHEMBL667262; (E,Z)-3-(4-(1,2-Diphenyl-1-butenyl)phenyl)-2-propenoic acid; (E)-3-[4-[(Z)-1,2-diphenylbut-1-enyl]phenyl]prop-2-enoic acid; BDBM50041611; GW5638; DPC 974; Q27460940; (E)-3-[4-((Z)-1,2-Diphenyl-but-1-enyl)-phenyl]-acrylic acid; (2E)-3-{4-[(1Z)-1,2-diphenylbut-1-en-1-yl]phenyl}prop-2-enoic acid; 2-Propenoic acid, 3-(4-(1,2-diphenyl-1-butenyl)phenyl)-, (E,Z)-

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Activity

IC50 ~ 100000 nM

[1]

Compound Name

2-[(1R,3R)-1-(4-Chlorophenyl)-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-2-yl]ethanol

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Investigative

Compound Info

Synonyms

CHEMBL3622994; BDBM50125085; (1R,3R)-1-(4-Chlorophenyl)-3-methyl-1,2,3,4-tetrahydro-beta-carboline-2-ethanol

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Activity

IC50 ~ 100000 nM

[1]

Compound Name

(E)-3-[4-[(1R,3R)-2-[(2S)-3-Hydroxy-2-methylpropyl]-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]phenyl]prop-2-enoic acid

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Investigative

Compound Info

Synonyms

CHEMBL3622999; BDBM50125079

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Activity

IC50 ~ 100000 nM

[1]

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References

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REF 1

Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist. J Med Chem. 2015 Oct 22;58(20):8128-40.

REF 2

6-arylcoumarins as novel nonsteroidal type progesterone antagonists: an example with receptor-binding-dependent fluorescence. J Med Chem. 2011 Oct 27;54(20):7055-65.

REF 3

Progesterone receptor antagonists with a 3-phenylquinazoline-2,4-dione/2-phenylisoquinoline-1,3-dione skeleton. Bioorg Med Chem. 2008 Jul 15;16(14):7046-54.

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