Target Poor or Non Binder(s) Information
Target General Information | Top | ||||
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Target ID | T48940 | Target Info | |||
Target Name | HIF-prolyl hydroxylase (HPH) | ||||
Target Type | Successful Target | ||||
Gene Name | NO-GeName | ||||
UniProt ID |
Poor Binders of This Target (in total, 15 binders) | Download | Top | |||
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Compound Name |
(12'S)-Bisbakuchiol C
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Investigative | Compound Info | ||
Synonyms |
CHEMBL258478; (12''''S)-Bisbakuchiol C; BDBM50478310
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Activity |
IC50 ~ 50000 nM
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[1] | |||
Compound Name |
12,13-Epoxybakuchiol
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Investigative | Compound Info | ||
Synonyms |
CHEMBL405046; 2,3-Epoxybakuchiol; BDBM50478314
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Activity |
IC50 ~ 50000 nM
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[1] | |||
Compound Name |
12,13-Diolbakuchiol
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Investigative | Compound Info | ||
Synonyms |
CHEMBL261315; BDBM50478309
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Activity |
IC50 ~ 50000 nM
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[1] | |||
Compound Name |
[5-(1-Benzylimidazo[1,5-a]pyridin-3-yl)furan-2-yl]methanol
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Investigative | Compound Info | ||
Synonyms |
CHEMBL3892315; BDBM50204477
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Activity |
IC50 = 56000 nM
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[2] | |||
Compound Name |
[5-[1-(4-Methoxyphenyl)imidazo[1,5-a]pyridin-3-yl]furan-2-yl]methanol
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Investigative | Compound Info | ||
Synonyms |
CHEMBL3918408; BDBM50204494
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Activity |
IC50 = 61000 nM
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[2] | |||
Compound Name |
[5-(1-Phenylimidazo[1,5-a]pyridin-3-yl)furan-2-yl]methanol
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Investigative | Compound Info | ||
Synonyms |
CHEMBL3961295; BDBM50204470
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Activity |
IC50 = 70000 nM
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[2] | |||
Compound Name |
4-[[5-[(3,5-Dimethylpyrazol-1-yl)methyl]furan-2-carbonyl]amino]-1H-pyrazole-5-carboxamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL3403038; BDBM50498111
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Activity |
IC50 = 71600 nM
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[3] | |||
Compound Name |
4-[[3-[(3,5-Dimethylpyrazol-1-yl)methyl]benzoyl]amino]-1-ethylpyrazole-3-carboxamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL3403035; BDBM50498116
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Activity |
IC50 = 72000 nM
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[3] | |||
Compound Name |
[5-[1-(2-Methoxyphenyl)imidazo[1,5-a]pyridin-3-yl]furan-2-yl]methanol
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Investigative | Compound Info | ||
Synonyms |
CHEMBL3940432; BDBM50204474
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Activity |
IC50 = 75000 nM
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[2] | |||
Compound Name |
1-Ethyl-4-[[5-(pyrazol-1-ylmethyl)furan-2-carbonyl]amino]pyrazole-3-carboxamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL3403041; BDBM50498110
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Activity |
IC50 = 81800 nM
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[3] | |||
Compound Name |
4-[[5-[(3,5-Dimethyl-1,2-oxazol-4-yl)methyl]furan-2-carbonyl]amino]-1-ethylpyrazole-3-carboxamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL3403042; BDBM50498109; ZINC28243319; MCULE-6484558696
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Activity |
IC50 ~ 100000 nM
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[3] | |||
Compound Name |
4-[[5-[(3,5-Dimethylpyrazol-1-yl)methyl]furan-2-carbonyl]amino]-1-ethyl-N,N-dimethylpyrazole-3-carboxamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL3403037; BDBM50498112
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Activity |
IC50 ~ 100000 nM
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[3] | |||
Compound Name |
5-[(3,5-Dimethylpyrazol-1-yl)methyl]-N-(4-oxo-6,7-dihydro-5H-pyrazolo[1,5-a]pyrazin-3-yl)furan-2-carboxamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL3403040; BDBM50498115
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Activity |
IC50 ~ 100000 nM
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[3] | |||
Compound Name |
4-[({5-[(3,5-Dimethyl-1H-pyrazol-1-yl)methyl]furan-2-yl}carbonyl)amino]-1-ethyl-1H-pyrazole-5-carboxamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL3403039; Oprea1_153271; BDBM50498107; STK304210; AKOS003759559
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Activity |
IC50 ~ 100000 nM
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[3] | |||
Compound Name |
4-[[5-[(3,5-Dimethylpyrazol-1-yl)methyl]thiophene-2-carbonyl]amino]-1-ethylpyrazole-3-carboxamide
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Investigative | Compound Info | ||
Synonyms |
CHEMBL3403034; BDBM50498113
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Activity |
IC50 ~ 100000 nM
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[3] | |||
Click to Show/Hide the Information of All Poor Binders |
Non Binders of This Target (in total, 4 non binders) | Download | Top | |||
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Compound Name |
(5S,7R)-7-(3-Bromo-2,6-difluorophenyl)-5-(3-bromophenyl)-4,5,6,7-tetrahydrotetrazolo[1,5-a]pyrimidine
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Investigative | Compound Info | ||
Synonyms |
CHEMBL3597782; SCHEMBL15739999; BDBM50105306
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Activity |
IC50 = 3800000 nM
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[4] | |||
Compound Name |
(2R)-1-[3-[2-(3,4-Dimethoxyphenyl)-2-oxoethoxy]-4-methoxyphenyl]-2-[4-[(2S,3R,4R,5S)-5-[4-[(2R)-1-[3-[2-(3,4-dimethoxyphenyl)-2-oxoethoxy]-4-methoxyphenyl]-1-oxopropan-2-yl]oxy-3-methoxyphenyl]-3,4-dimethyloxolan-2-yl]-2-methoxyphenoxy]propan-1-one
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Investigative | Compound Info | ||
Synonyms |
CHEMBL3623804; BDBM50498798
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Activity |
IC50 > 10000000 nM
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[5] | |||
Compound Name |
(5S,7R)-5-(3-Bromo-5-fluorophenyl)-7-(3-bromophenyl)-4,5,6,7-tetrahydrotetrazolo[1,5-a]pyrimidine
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Investigative | Compound Info | ||
Synonyms |
CHEMBL3597786; SCHEMBL15740053; BDBM50105310; (5S,7R)-5-(3-bromo-5-fluorophenyl)-7-(3-bromophenyl)-1,5,6,7-tetrahydrotetrazolo[1,5-a]pyrimidine
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Activity |
IC50 = 14500000 nM
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[4] | |||
Compound Name |
(5S,7R)-5-(3-Bromophenyl)-7-(2-bromophenyl)-4,5,6,7-tetrahydrotetrazolo[1,5-a]pyrimidine
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Investigative | Compound Info | ||
Synonyms |
CHEMBL3597694; BDBM50105272
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Activity |
IC50 = 18900000 nM
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[4] |
References | Top | ||||
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REF 1 | Hypoxia-inducible factor-1 and nuclear factor-kappaB inhibitory meroterpene analogues of bakuchiol, a constituent of the seeds of Psoralea corylifolia. Bioorg Med Chem Lett. 2008 Apr 15;18(8):2619-23. | ||||
REF 2 | Development of 1-aryl-3-furanyl/thienyl-imidazopyridine templates for inhibitors against hypoxia inducible factor (HIF)-1 transcriptional activity. Bioorg Med Chem Lett. 2016 Dec 15;26(24):5887-5890. | ||||
REF 3 | Design, synthesis, and structure-activity relationships of 1-ethylpyrazole-3-carboxamide compounds as novel hypoxia-inducible factor (HIF)-1 inhibitors. Bioorg Med Chem. 2015 Apr 15;23(8):1776-87. | ||||
REF 4 | Isoform-Selective and Stereoselective Inhibition of Hypoxia Inducible Factor-2. J Med Chem. 2015 Aug 13;58(15):5930-41. | ||||
REF 5 | Synthesis and Biological Evaluation of Manassantin Analogues for Hypoxia-Inducible Factor 1alpha Inhibition. J Med Chem. 2015 Oct 8;58(19):7659-71. |
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