Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T41145 | Target Info | |||
| Target Name | Bromodomain and PHD finger containing 1 (BRPF1) | ||||
| Synonyms |
Protein Br140; Peregrin; Bromodomain and PHD finger-containing protein 1; BR140
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| Target Type | Literature-reported Target | ||||
| Gene Name | BRPF1 | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 9 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Chembl4280229
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Investigative | Compound Info | ||
| Synonyms |
BDBM50468523; ZINC14247397; AKOS034652861; MCULE-4383264866; Z88259959
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
Chembl4284079
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Investigative | Compound Info | ||
| Synonyms |
BDBM50468500
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
Chembl4288422
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Investigative | Compound Info | ||
| Synonyms |
BDBM50468554; ZINC48288205; AKOS034304896; MCULE-6162620667; Z422219284
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
Chembl4277110
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Investigative | Compound Info | ||
| Synonyms |
BDBM50468506; ZINC18132336; AKOS034492101; MCULE-4759778995; Z62928064
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
4-Cyano-N-(1,3-diethyl-2-oxoquinolin-6-yl)benzenesulfonamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4059509; BDBM50249797
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| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
Chembl4289781
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Investigative | Compound Info | ||
| Synonyms |
BDBM50468522; AKOS034199824; MCULE-6197853530; Z335384138
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
Chembl4213809
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Investigative | Compound Info | ||
| Synonyms |
BDBM50455493; D7H
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|
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
Chembl4291947
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|
Investigative | Compound Info | ||
| Synonyms |
BDBM50468551; ZINC16777811; AKOS033043170; MCULE-8426507038; Z109815900
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
Chembl4281624
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|
Investigative | Compound Info | ||
| Synonyms |
BDBM50468540; AKOS033789423; MCULE-1677473771; Z218342380; 3,5-dimethyl-N-{4-[(3-methylpiperidin-1-yl)methyl]-1,3-thiazol-2-yl}-1,2-oxazole-4-carboxamide
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|
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| Activity |
IC50 = 195000 nM
|
[1] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 12 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Chembl4283908
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|
Investigative | Compound Info | ||
| Synonyms |
BDBM50468497; AKOS002121956; MCULE-9901523982
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| Activity |
IC50 > 200000 nM
|
[1] | |||
| Compound Name |
Chembl4288352
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Investigative | Compound Info | ||
| Synonyms |
BDBM50468528; CCG-154867; MCULE-7718035397; 6-{[2-(4-chlorophenyl)pyrrolidin-1-yl]sulfonyl}-1,4-dimethyl-1,4-dihydroquinoxaline-2,3-dione
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| Activity |
IC50 > 200000 nM
|
[1] | |||
| Compound Name |
Chembl4282321
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Investigative | Compound Info | ||
| Synonyms |
BDBM50468547; ZINC45994469; MCULE-1557432538
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| Activity |
IC50 > 200000 nM
|
[1] | |||
| Compound Name |
Chembl4292260
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Investigative | Compound Info | ||
| Synonyms |
BDBM50468545
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| Activity |
IC50 > 200000 nM
|
[1] | |||
| Compound Name |
Chembl4281952
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Investigative | Compound Info | ||
| Synonyms |
BDBM50468507; EiM08-15423; STK937673; STL469331; ZINC44903042; AKOS005666974; AKOS016374564; MCULE-9651274937
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| Activity |
IC50 > 200000 nM
|
[1] | |||
| Compound Name |
Chembl4292561
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Investigative | Compound Info | ||
| Synonyms |
ZINC6767537; BDBM50468544; STL479741; AKOS001882555; MCULE-5991228636; 2,4-dimethyl-N-(4-piperidin-1-ylphenyl)-1,3-thiazole-5-carboxamide; 2,4-dimethyl-N-[4-(piperidin-1-yl)phenyl]-1,3-thiazole-5-carboxamide
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|
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| Activity |
IC50 = 218000 nM
|
[1] | |||
| Compound Name |
Chembl4288853
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Investigative | Compound Info | ||
| Synonyms |
BDBM50468541; AKOS033789741; MCULE-6614285587; Z218453136; 4-methyl-N-{4-[(3-methylpiperidin-1-yl)methyl]-1,3-thiazol-2-yl}-1,2,3-thiadiazole-5-carboxamide
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| Activity |
IC50 = 240000 nM
|
[1] | |||
| Compound Name |
Chembl4282346
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Investigative | Compound Info | ||
| Synonyms |
BDBM50468542; Z1926609871; 7-oxo-N-{4-[(piperidin-1-yl)methyl]-1,3-thiazol-2-yl}azepane-2-carboxamide
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| Activity |
IC50 = 293000 nM
|
[1] | |||
| Compound Name |
1,4-Dimethylquinoxaline-2,3-dione
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Investigative | Compound Info | ||
| Synonyms |
1,4-dimethyl-1,4-dihydroquinoxaline-2,3-dione; CHEMBL4281139; 1,4-DIMETHYLQUINOXALINE-2,3(1H,4H)-DIONE; 1,4-Dimethyl-1,4-dihydro-quinoxaline-2,3-dione; 2,3-Quinoxalinedione,1,4-dihydro-1,4-dimethyl-; NSC521681; SCHEMBL1278798; CTK5A7957; ZINC15173; DTXSID10325897; BDBM50468536; SBB006357; STK129623; AKOS003277876; CCG-356217; MCULE-1046503849; NSC-521681; ST057487; 1,4-dimethylquinoxaline-2,3(1H,4H)dione; 1,4-dimethylquinoxaline-2,3 (1H,4H)-dione; 1,4-Dihydro-1,4-dimethyl-2,3-quinoxalinedione; A831769; 1,4-dimethyl-1,2,3,4-tetrahydroquinoxaline-2,3-dione
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| Activity |
IC50 > 400000 nM
|
[1] | |||
| Compound Name |
Chembl4278478
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Investigative | Compound Info | ||
| Synonyms |
BDBM50468498; ZINC95977957; AKOS033416541; MCULE-1220734577; Z1544661863; 3-methyl-N-{4-[(morpholin-4-yl)methyl]-1,3-thiazol-2-yl}-5-(propan-2-yl)-1H-pyrazole-4-carboxamide
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| Activity |
IC50 > 500000 nM
|
[1] | |||
| Compound Name |
Chembl4294159
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Investigative | Compound Info | ||
| Synonyms |
BDBM50468555; AKOS034496449; MCULE-5437110630; Z642045762; N-{4-[(3,5-dimethylpiperidin-1-yl)methyl]-1,3-thiazol-2-yl}-4-methyl-1,3-thiazole-5-carboxamide
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|
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| Activity |
IC50 > 500000 nM
|
[1] | |||
| Compound Name |
Chembl4289143
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|
Investigative | Compound Info | ||
| Synonyms |
BDBM50468543
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|
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| Activity |
IC50 = 515000 nM
|
[1] | |||
| Click to Show/Hide the Information of All Non Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Structure-based discovery of selective BRPF1 bromodomain inhibitors. Eur J Med Chem. 2018 Jul 15;155:337-352. | ||||
| REF 2 | Design of a Chemical Probe for the Bromodomain and Plant Homeodomain Finger-Containing (BRPF) Family of Proteins. J Med Chem. 2017 Aug 24;60(16):6998-7011. | ||||
| REF 3 | Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain. J Med Chem. 2018 May 24;61(10):4317-4334. | ||||
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