Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T21123 | Target Info | |||
| Target Name | Hypoxia-inducible factor 2 alpha (HIF-2A) | ||||
| Synonyms |
bHLHe73; PASD2; PAS domain-containing protein 2; Member of PAS protein 2; MOP2; Hypoxia-inducible factor 2-alpha; HLF; HIF2A; HIF2-alpha; HIF-2-alpha; HIF-1-alpha-like factor; Endothelial PAS domain-containing protein 1; EPAS-1; Class E basic helix-loop-helix protein 73; Basic-helix-loop-helix-PAS protein MOP2
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| Target Type | Successful Target | ||||
| Gene Name | EPAS1 | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 9 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Chembl4163733
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Investigative | Compound Info | ||
| Synonyms |
SCHEMBL16555806; BDBM50450489
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| Activity |
IC50 = 52900 nM
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[1] | |||
| Compound Name |
Chembl4159084
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Investigative | Compound Info | ||
| Synonyms |
BDBM50450498
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| Activity |
IC50 ~ 100000 nM
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[1] | |||
| Compound Name |
7-Methoxy-1,2,6-trimethylisoquinoline-3,5,8-trione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL509316; BDBM50398331
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| Activity |
EC50 ~ 100000 nM
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[2] | |||
| Compound Name |
Aaptamine
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Investigative | Compound Info | ||
| Synonyms |
UNII-FGW9D01COE; 8,9-dimethoxy-1H-benzo[de][1,6]naphthyridine; FGW9D01COE; 1H-Benzo(de)(1,6)naphthyridine, 8,9-dimethoxy-; 8,9-Dimethoxy-1H-benzo(de)(1,6)naphthyridine; 1H-benzo[de][1,6]naphthyridine, 8,9-dimethoxy-; BRN 3550089; 8,9-dimethoxy-4h-benzo[de][1,6]naphthyridine; CHEMBL234658; SCHEMBL8024280; CTK5F5187; DTXSID201006106; HY-N4225; BDBM50356012; AKOS027381877; ZINC100152478; SMP2_000065; CS-0032464; Q5682186
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| Activity |
EC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
Xestoquinone
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Investigative | Compound Info | ||
| Synonyms |
(+)-Xestoquinone; 1-XQN; CHEMBL510492; SCHEMBL12104111; DTXSID90913675; BDBM50398330; NSC643406; NSC-643406; NCI60_014669; C20073; Q15634140; 12b-Methyl-2,3-dihydro-1H-tetrapheno[5,4-bc]furan-6,8,11(12bH)-trione; (S)-12b-Methyl-2,3-dihydro-1H-tetrapheno[5,4-bc]furan-6,8,11(12bH)-trione
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| Activity |
EC50 ~ 100000 nM
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[2] | |||
| Compound Name |
[(1S,2R,5S,10R,11S,13R,16S,17S,18S,20S)-17-Acetyl-18-hydroxy-2,6,6,20-tetramethyl-15-oxo-14-oxapentacyclo[11.6.1.02,11.05,10.016,20]icosan-10-yl]methyl acetate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL508487; BDBM50398323
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| Activity |
EC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
(1R,3S,14S)-6,10,14-Trimethyl-3-(prop-1-en-2-yl)-15-oxabicyclo[12.1.0]pentadeca-6,10-dien-5-one
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1761948; BDBM50340946
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| Activity |
EC50 = 107500 nM
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[3] | |||
| Compound Name |
(1R,4E,6E,10E,14S)-7-(2-Methoxypropan-2-yl)-4,10,14-trimethyl-15-oxabicyclo[12.1.0]pentadeca-4,6,10-triene
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1761952; BDBM50340948
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| Activity |
EC50 = 148900 nM
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[3] | |||
| Compound Name |
(1R,2E,6R,8S,11E)-3,8,12,16-Tetramethyl-7,18-dioxatricyclo[13.3.0.06,8]octadeca-2,11,15-triene
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1761950; BDBM50340947; (6R,8S,18R)-3,8,12,16-Tetramethyl-7,18-dioxa-tricyclo[13.3.0.0*6,8*]octadeca-2,11,15-triene
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| Activity |
EC50 = 183300 nM
|
[3] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Design and Activity of Specific Hypoxia-Inducible Factor-2alpha (HIF-2alpha) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate ( S)-3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1 H-inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385). J Med Chem. 2018 Nov 8;61(21):9691-9721. | ||||
| REF 2 | Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges. J Nat Prod. 2012 Sep 28;75(9):1632-6. | ||||
| REF 3 | Identification and evaluation of soft coral diterpenes as inhibitors of HIF-2alpha induced gene expression. Bioorg Med Chem Lett. 2011 Apr 1;21(7):2113-5. | ||||
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