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Found 2448 with Last Name = 'pio' and Initial = 'b'
TargetAndrogen receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

LigandPNGBDBM18161((1S,2S,7S,10R,11S,14S,15S)-14-hydroxy-2,15-dimethy...)
Affinity DataKi:  0.200nM EC50:  5.10nMAssay Description:The compounds were evaluated in a transcriptional activation assay with hAR in a mammalian cell background (CV-1) as the primary in vitro assay. Rece...More data for this Ligand-Target Pair
TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50129152((6S,8S,10R,14S,15S)-17-Acetyl-6,10-dimethyl-13-(R)...)
Affinity DataKi:  0.340nMAssay Description:Binding affinity to human progesterone receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50067678((6alpha)-17-(Acetyloxy)-6-methylpreg-4-ene-3,20-di...)
Affinity DataKi:  0.340nMAssay Description:Binding affinity towards human progesterone receptor A isoform using progesterone as radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50133141(9-Fluoro-2,2,4-trimethyl-5-[1-(3-methyl-pyridin-2-...)
Affinity DataKi:  0.420nMAssay Description:Binding affinity towards human progesterone receptor A isoform using progesterone as radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50133131(9-Fluoro-2,2,4-trimethyl-5-[1-o-tolyl-meth-(Z)-yli...)
Affinity DataKi:  0.550nMAssay Description:Binding affinity towards human progesterone receptor A isoform using progesterone as radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50133135(9-Fluoro-2,2,4-trimethyl-5-[1-(2-methylsulfanyl-ph...)
Affinity DataKi:  0.590nMAssay Description:Binding affinity towards human progesterone receptor A isoform using progesterone as radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50133146(7-Fluoro-2,2,4-trimethyl-5-[1-phenyl-meth-(Z)-ylid...)
Affinity DataKi:  0.610nMAssay Description:Binding affinity towards human progesterone receptor A isoform using progesterone as radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50133139(9-Fluoro-5-[1-(2-fluoro-phenyl)-meth-(Z)-ylidene]-...)
Affinity DataKi:  0.620nMAssay Description:Binding affinity towards human progesterone receptor A isoform using progesterone as radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50133152(9-Fluoro-2,2,4-trimethyl-5-[1-phenyl-meth-(Z)-ylid...)
Affinity DataKi:  0.620nMAssay Description:Binding affinity towards human progesterone receptor A isoform using progesterone as radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50067684(2,2,4-Trimethyl-5-[1-o-tolyl-meth-(Z)-ylidene]-2,5...)
Affinity DataKi:  0.660nMAssay Description:Binding affinity towards human progesterone receptor A isoform using progesterone as radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50067684(2,2,4-Trimethyl-5-[1-o-tolyl-meth-(Z)-ylidene]-2,5...)
Affinity DataKi:  0.660nMAssay Description:Binding affinity to human progesterone receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50133143(7-Fluoro-5-[1-(4-fluoro-phenyl)-meth-(Z)-ylidene]-...)
Affinity DataKi:  0.710nMAssay Description:Binding affinity towards human progesterone receptor A isoform using progesterone as radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataKi:  1.10nMAssay Description:Binding affinity at human progesterone receptor.More data for this Ligand-Target Pair
TargetProthrombin(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM252994(US9469608, 23-4b)
Affinity DataKi:  1.10nMpH: 7.4Assay Description:Relevant in vitro assays are referenced in Morrissette, et al., Bioorg. Med. Chem. Lett. 2004, 14, 4161-4164 and described in Lewis, et al. Thromb. R...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataKi:  1.10nMAssay Description:Binding affinity to human progesterone receptorMore data for this Ligand-Target Pair
TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50133151(CHEMBL336353 | {2-[9-Fluoro-2,2,4-trimethyl-1,2-di...)
Affinity DataKi:  1.20nMAssay Description:Binding affinity towards human progesterone receptor A isoform using progesterone as radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50133140(9-Fluoro-2,2,4-trimethyl-5-[1-thiophen-3-yl-meth-(...)
Affinity DataKi:  1.30nMAssay Description:Binding affinity towards human progesterone receptor A isoform using progesterone as radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50133153(9-Fluoro-2,2,4-trimethyl-5-[1-(3-methyl-pyridin-4-...)
Affinity DataKi:  1.40nMAssay Description:Binding affinity towards human progesterone receptor A isoform using progesterone as radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50133133(7-Fluoro-2,2,4-trimethyl-5-[1-o-tolyl-meth-(Z)-yli...)
Affinity DataKi:  1.5nMAssay Description:Binding affinity towards human progesterone receptor A isoform using progesterone as radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50133150(9-Fluoro-2,2,4-trimethyl-5-[1-pyridin-4-yl-meth-(Z...)
Affinity DataKi:  1.5nMAssay Description:Binding affinity towards human progesterone receptor A isoform using progesterone as radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50133147(9-Fluoro-2,2,4-trimethyl-5-[1-(2-propyl-phenyl)-me...)
Affinity DataKi:  1.60nMAssay Description:Binding affinity towards human progesterone receptor A isoform using progesterone as radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50133138(9-Fluoro-5-[1-(2-isopropyl-phenyl)-meth-(Z)-yliden...)
Affinity DataKi:  1.90nMAssay Description:Binding affinity towards human progesterone receptor A isoform using progesterone as radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50129146((Z)-5-(bromomethylene)-9-fluoro-2,2,4-trimethyl-2,...)
Affinity DataKi:  2.10nMAssay Description:Binding affinity to human progesterone receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50133136(5-[1-(2-Ethyl-phenyl)-meth-(Z)-ylidene]-9-fluoro-2...)
Affinity DataKi:  2.30nMAssay Description:Binding affinity towards human progesterone receptor A isoform using progesterone as radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50129145(9-Fluoro-2,2,4-trimethyl-5-((Z)-3-methyl-but-2-eny...)
Affinity DataKi:  2.5nMAssay Description:Binding affinity for human progesterone receptor; Not activeMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM253008(US9469608, 36-3)
Affinity DataKi:  2.5nMpH: 7.4Assay Description:Relevant in vitro assays are referenced in Morrissette, et al., Bioorg. Med. Chem. Lett. 2004, 14, 4161-4164 and described in Lewis, et al. Thromb. R...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetProthrombin(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM253006(US9469608, 34-7)
Affinity DataKi:  2.5nMpH: 7.4Assay Description:Relevant in vitro assays are referenced in Morrissette, et al., Bioorg. Med. Chem. Lett. 2004, 14, 4161-4164 and described in Lewis, et al. Thromb. R...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50086537(2,2,4-Trimethyl-6-(5-nitro-thiophen-2-yl)-1,2-dihy...)
Affinity DataKi:  2.60nMAssay Description:Binding affinity against human progesterone receptor (hPR) in a competitive binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50133130(2-[9-Fluoro-2,2,4-trimethyl-1,2-dihydro-6-oxa-1-az...)
Affinity DataKi:  2.60nMAssay Description:Binding affinity towards human progesterone receptor A isoform using progesterone as radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAndrogen receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

LigandPNGBDBM50067678((6alpha)-17-(Acetyloxy)-6-methylpreg-4-ene-3,20-di...)
Affinity DataKi:  2.90nMAssay Description:Inhibition of DHT binding to human androgen receptor expressed in baculovirus SF-12 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research And Development

Curated by ChEMBL
LigandPNGBDBM50179351((2-chloro-3-methyl-4H-thieno[3,2-b]pyrrol-5-yl)(4-...)
Affinity DataKi:  3nMAssay Description:Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProteinase-activated receptor 1(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM230675(US9340530, 13)
Affinity DataKi:  3nMpH: 7.5Assay Description:Thrombin receptor antagonists were screened using a modification of the thrombin receptor radioligand binding assay of Ahn et al. (Ahn et al., Mol. P...More data for this Ligand-Target Pair
Ligand InfoKEGGPC cidPC sid
In DepthDetails US Patent
TargetProteinase-activated receptor 1(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM230672(US9340530, 10)
Affinity DataKi:  3nMpH: 7.5Assay Description:Thrombin receptor antagonists were screened using a modification of the thrombin receptor radioligand binding assay of Ahn et al. (Ahn et al., Mol. P...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetProteinase-activated receptor 1(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM230664(US9340530, 2)
Affinity DataKi:  3nMpH: 7.5Assay Description:Thrombin receptor antagonists were screened using a modification of the thrombin receptor radioligand binding assay of Ahn et al. (Ahn et al., Mol. P...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50129144((Z)-5-butylidene-9-fluoro-2,2,4-trimethyl-2,5-dihy...)
Affinity DataKi:  3.10nMAssay Description:Binding affinity to human progesterone receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDimer of Gag-Pol polyprotein [489-587](Human immunodeficiency virus type 1)
Sandoz Research Institute

LigandPNGBDBM1226(2-Aminobenzyl-Substituted AHPPA deriv. 44 | benzyl...)
Affinity DataKi:  3.30nM IC50:  175nMAssay Description:Enzymatic activity was measured by following cleavage of the substrate H-Lys-Ala-Arg-Val-Leu-pNph-Glu-Ala-Nle-NH2. Products of the cleavage reaction ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDimer of Gag-Pol polyprotein [489-587](Human immunodeficiency virus type 1)
Sandoz Research Institute

LigandPNGBDBM964(2-Aminobenzyl-Substituted AHPPA deriv. 1 | 5PhBuCO...)
Affinity DataKi:  3.40nM ΔG°:  -50.3kJ/mole IC50:  25nMpH: 6.25 T: 2°CAssay Description:Enzymatic activity was measured by following cleavage of the substrate H-Lys-Ala-Arg-Val-Leu-pNph-Glu-Ala-Nle-NH2. Products of the cleavage reaction ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDimer of Gag-Pol polyprotein [489-587](Human immunodeficiency virus type 1)
Sandoz Research Institute

LigandPNGBDBM964(2-Aminobenzyl-Substituted AHPPA deriv. 1 | 5PhBuCO...)
Affinity DataKi:  3.40nMAssay Description:Enzymatic activity was measured by following cleavage of the substrate H-Lys-Ala-Arg-Val-Leu-pNph-Glu-Ala-Nle-NH2. Products of the cleavage reaction ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM253013(US9469608, 39-10b)
Affinity DataKi:  3.40nMpH: 7.4Assay Description:Relevant in vitro assays are referenced in Morrissette, et al., Bioorg. Med. Chem. Lett. 2004, 14, 4161-4164 and described in Lewis, et al. Thromb. R...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetProthrombin(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM253012(US9469608, 39-10a)
Affinity DataKi:  3.40nMpH: 7.4Assay Description:Relevant in vitro assays are referenced in Morrissette, et al., Bioorg. Med. Chem. Lett. 2004, 14, 4161-4164 and described in Lewis, et al. Thromb. R...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetProthrombin(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM252985(US9469608, 13-10)
Affinity DataKi:  3.40nMpH: 7.4Assay Description:Relevant in vitro assays are referenced in Morrissette, et al., Bioorg. Med. Chem. Lett. 2004, 14, 4161-4164 and described in Lewis, et al. Thromb. R...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM8903((1S,2R,10S,11S,14S,15S)-14-acetyl-2,15-dimethyltet...)
Affinity DataKi:  3.5nMAssay Description:Human progesterone receptor (hPR) agonist activity in T47D human breast cancer cell lineMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM8903((1S,2R,10S,11S,14S,15S)-14-acetyl-2,15-dimethyltet...)
Affinity DataKi:  3.5nMAssay Description:Binding affinity to human progesterone receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM8903((1S,2R,10S,11S,14S,15S)-14-acetyl-2,15-dimethyltet...)
Affinity DataKi:  3.5nMAssay Description:Binding affinity towards human progesterone receptor A isoform using progesterone as radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50086546(4-(2,2,4-Trimethyl-1,2-dihydro-quinolin-6-yl)-thio...)
Affinity DataKi:  3.5nMAssay Description:Antagonist activity against human progesterone receptor (hPR) in T47D human breast cancer cell lineMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50133144(9-Fluoro-5-[1-(2-methoxy-phenyl)-meth-(Z)-ylidene]...)
Affinity DataKi:  3.80nMAssay Description:Binding affinity towards human progesterone receptor A isoform using progesterone as radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM253004(US9469608, 32-7)
Affinity DataKi:  3.90nMpH: 7.4Assay Description:Relevant in vitro assays are referenced in Morrissette, et al., Bioorg. Med. Chem. Lett. 2004, 14, 4161-4164 and described in Lewis, et al. Thromb. R...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetProgesterone receptor(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50086550(4-Methyl-5-(2,2,4,4-tetramethyl-3-oxo-1,2,3,4-tetr...)
Affinity DataKi:  3.90nMAssay Description:Binding affinity against human progesterone receptor (hPR) in a competitive binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H4 receptor(Homo sapiens (Human))
Johnson & Johnson Pharmaceutical Research And Development

Curated by ChEMBL
LigandPNGBDBM22566(5-chloro-2-[(4-methylpiperazin-1-yl)carbonyl]-1H-i...)
Affinity DataKi:  4nMAssay Description:Displacement of [3H]histamine from recombinant human histamine H4 receptor in SK-N-MC cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDimer of Gag-Pol polyprotein [489-587](Human immunodeficiency virus type 1)
Sandoz Research Institute

LigandPNGBDBM1228(2-Aminobenzyl-Substituted AHPPA deriv. 46 | benzyl...)
Affinity DataKi:  4.10nM IC50:  161nMAssay Description:Enzymatic activity was measured by following cleavage of the substrate H-Lys-Ala-Arg-Val-Leu-pNph-Glu-Ala-Nle-NH2. Products of the cleavage reaction ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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