Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T30790 | Target Info | |||
| Target Name | Calcium-release activated calcium channel (CRACM) | ||||
| Synonyms |
Transmembrane protein 142A; TMEM142A; Protein orai-1; Calcium release-activated calcium channel protein 1; CRACM1
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| Target Type | Clinical trial Target | ||||
| Gene Name | ORAI1 | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 18 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Econazole
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Approved | Compound Info | ||
| Synonyms |
Ecostatin; Palavale; Pevaryl; Ecostatin Vaginal Ovules; Ecostatin cream; Spectazole cream; SQ 13050; Ecostatin (TN); Gyno-Pevaryl 150; Gyno-pevaryl; Pevaryl (TN); Spectazole (TN); Econazole (USAN/INN); 1-[2,4-Dichloro-.beta.-[(p-chlorobenzyl)oxy]phenethyl]imidazole; 1-[2-[(4-Chlorophenyl)methoxy]-2-(2,4-dichlorophenyl)ethyl]-1H-imidazole; 1-[2-[(4-chlorophenyl)methoxy]-2-(2,4-dichlorophenyl)ethyl]imidazole; 1-{2-(4-chlorobenzyloxy)-2-(2,4-dichlorophenyl)ethyl}-1H-imidazole; 1-{2-[(4-chlorobenzyl)oxy]-2-(2,4-dichlorophenyl)ethyl}-1H-imidazole; 1-{2-[(4-chlorophenyl)methoxy]-2-(2,4-dichlorophenyl)ethyl}-1H-imidazole
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| Activity |
IC50 = 94000 nM
|
[1] | |||
| Compound Name |
Miconazole
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Approved | Compound Info | ||
| Synonyms |
Dactarin; MCZ; Miconazol; Miconazolo; Miconazolum; Micozole; Minostate; Monistat; Vusion; Zimycan; Daktarin IV; Miconasil Nitrate; Miconazole nitrate salt; Miconazolo [DCIT]; Monistat IV; MJR 1762; Miconazole 3; Miconazole 3 Combination Pack; Miconazole 7 Combination Pack; Monazole 7; Monistat 1 Combination Pack; Monistat 3 Vaginal Ovules; Monistat 5 Tampon; Monistat 7 Vaginal Suppositories; R 18134; Aflorix(nitrate); Albistat(nitrate); Andergin(nitrate); Conofite(nitrate); Daktarin (TN); Femizol (TN); Femizol-M; Florid(nitrate); Lotrimin AF(nitrate); Micantin (nitrate); Micatin (TN); Miconazex (TN); Miconazol [INN-Spanish]; Miconazole-7; Miconazolum [INN-Latin]; Monista (nitrate); Monistat (TN); Monistat 3 Dual-Pak; Monistat 7 Dual-Pak; Monistat Dual-PAK; Monistat iv (TN); Monistat-Derm; Novo-Miconazole Vaginal Ovules; Epi-Monistat(nitrate); Gyno-Daktar(nitrate); Monistat-Derm (TN); R-14,889; Miconazole (JP15/USP/INN); Miconazole [USAN:BAN:INN:JAN]; Imidazole, 1-(2-(2,4-dichlorophenyl)-2-((2,4-dichlorophenyl) methoxy)ethyl)-(9CI); Imidazole, 1-(2-(2,4-dichlorophenyl)-2-((2,4-dichlorophenyl)methoxy)ethyl)-(9CI); (+-)-1-(2,4-Dichloro-beta-((2,4-dichlorobenzyl)oxy)phenethyl)imidazole; 1-(2,4-Dichloro-beta-((2,4-dichlorobenzyl)oxy)phenethyl)imidazole; 1-(2,4-dichloro-beta-((2,4-dichlorobenzyl)oxy)phenethyl) imidazole; 1-[2,4-Dichloro-beta-([2,4-dichloro-benzyl]oxy)phenethyl]imidazole; 1-[2-(2,4-Dichlorophenyl)-2-[(2,4-dichlorophenyl)methoxy]ethyl]-1H-imidazole; 1-[2-(2,4-dichlorobenzyloxy)-2-(2,4-dichlorophenyl)ethyl]-1H-imidazole; 1-[2-(2,4-dichlorophenyl)-2-[(2,4-dichlorophenyl)methoxy]ethyl]imidazole; 1-[2-(2,4-dichlorophenyl)-2-{[(2,4-dichlorophenyl)methyl]oxy}ethyl]-1H-imidazole; 1-{2-[(2,4-dichlorobenzyl)oxy]-2-(2,4-dichlorophenyl)ethyl}-1H-imidazole
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| Activity |
IC50 = 100000 nM
|
[1] | |||
| Compound Name |
Mibefradil
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Phase 1 | Compound Info | ||
| Synonyms |
Mibefradil (Cytostatic Checkpoint Therapy, ovarian cancer); Mibefradil (Cytostatic Checkpoint Therapy, ovarian cancer), Tau Therapeutics; Calcium T-channel inhibitor (Cytostatic Checkpoint Therapy, ovarian cancer), Tau Therapeutics
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| Activity |
IC50 = 52100 nM
|
[1] | |||
| Compound Name |
Chembl4128097
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Investigative | Compound Info | ||
| Synonyms |
BDBM50273598
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| Activity |
IC50 = 54000 nM
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[2] | |||
| Compound Name |
Chembl4126055
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Investigative | Compound Info | ||
| Synonyms |
BDBM50273596
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| Activity |
IC50 = 55000 nM
|
[2] | |||
| Compound Name |
Chembl4130134
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Investigative | Compound Info | ||
| Synonyms |
BDBM50273557
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| Activity |
IC50 = 55000 nM
|
[2] | |||
| Compound Name |
N-[4-[3,5-Bis(trifluoromethyl)pyrazol-1-yl]phenyl]-4-chlorobenzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL100350; N-(4-(3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl)phenyl)-4-chlorobenzamide; SCHEMBL5208645; ZINC3129506; BDBM50204537; CCG-246724; MCULE-4275029748; 4-chloro-4'-[3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl]benzanilide; 4-chloro-4'-[ 3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl]benzanilide; N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazole-1-yl]phenyl]-4-chlorobenzamide
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| Activity |
IC50 = 57000 nM
|
[1] | |||
| Compound Name |
Chembl4126724
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Investigative | Compound Info | ||
| Synonyms |
BDBM50273586
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| Activity |
IC50 = 58000 nM
|
[2] | |||
| Compound Name |
Chembl4128127
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Investigative | Compound Info | ||
| Synonyms |
BDBM50273614
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| Activity |
IC50 = 60000 nM
|
[2] | |||
| Compound Name |
1-(4-Methoxyphenyl)-2-(1H-imidazole-1-yl)ethyl 4-(4-methoxyphenyl)butyl ether
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3913392; BDBM50204538; J3.603.308H
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| Activity |
IC50 = 67000 nM
|
[1] | |||
| Compound Name |
(E)-1-[2-[2-(4-Butan-2-ylphenoxy)ethoxy]-3,5-dichlorophenyl]-N-(1,2,4-triazol-4-yl)methanimine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3907105; BDBM50204540
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| Activity |
IC50 = 69900 nM
|
[1] | |||
| Compound Name |
2-(4-Methoxyphenoxy)-1-[4-(4-phenylcyclohexyl)piperazin-1-yl]ethanone
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1545070; 1-[(4-methoxyphenoxy)acetyl]-4-(4-phenylcyclohexyl)piperazine; MLS000683423; HMS2608E12; BDBM50204543; STK194193; ZINC19790036; AKOS003650739; SMR000267946; AT-057/43316659
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| Activity |
IC50 = 75000 nM
|
[1] | |||
| Compound Name |
Chembl4129650
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Investigative | Compound Info | ||
| Synonyms |
BDBM50273569
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| Activity |
IC50 = 75000 nM
|
[2] | |||
| Compound Name |
Chembl4128278
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Investigative | Compound Info | ||
| Synonyms |
BDBM50273584
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| Activity |
IC50 = 79000 nM
|
[2] | |||
| Compound Name |
Chembl4129353
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Investigative | Compound Info | ||
| Synonyms |
BDBM50273560
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| Activity |
IC50 = 89000 nM
|
[2] | |||
| Compound Name |
Chembl4127069
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Investigative | Compound Info | ||
| Synonyms |
BDBM50273605
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| Activity |
IC50 = 89000 nM
|
[2] | |||
| Compound Name |
3,5-Dichloro-2-(2-pyridin-3-yloxyethoxy)benzaldehyde
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3972536; BDBM50204535
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| Activity |
IC50 = 100000 nM
|
[1] | |||
| Compound Name |
Chembl4128236
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Investigative | Compound Info | ||
| Synonyms |
BDBM50273615
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| Activity |
IC50 = 105000 nM
|
[2] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Evaluation of known and novel inhibitors of Orai1-mediated store operated Ca 2+ entry in MDA-MB-231 breast cancer cells using a Fluorescence Imaging Plate Reader assay. Bioorg Med Chem. 2017 Jan 1;25(1):440-449. | ||||
| REF 2 | An SAR study of hydroxy-trifluoromethylpyrazolines as inhibitors of Orai1-mediated store operated Ca 2+ entry in MDA-MB-231 breast cancer cells using a convenient Fluorescence Imaging Plate Reader assay. Bioorg Med Chem. 2018 Jul 23;26(12):3406-3413. | ||||
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