Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T43548 | Target Info | |||
| Target Name | B-cell lymphoma 6 protein (BCL-6) | ||||
| Synonyms |
Zinc finger protein 51; Zinc finger and BTB domain-containing protein 27; ZNF51; ZBTB27; Protein LAZ-3; LAZ3; BCL5; BCL-6; BCL-5; B-cell lymphoma 5 protein
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| Target Type | Literature-reported Target | ||||
| Gene Name | BCL6 | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 10 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
N-[4-[3-Cyano-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidin-5-yl]-2-[(3R)-3-(dimethylamino)pyrrolidin-1-yl]phenyl]acetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4065661
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| Activity |
IC50 = 61000 nM
|
[1] | |||
| Compound Name |
Chembl4171221
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Investigative | Compound Info | ||
| Synonyms |
BDBM50366291
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| Activity |
IC50 = 62000 nM
|
[2] | |||
| Compound Name |
2-[(2S)-1-[3-Cyano-7-(cyclopropylamino)pyrazolo[1,5-a]pyrimidin-5-yl]pyrrolidin-2-yl]acetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4089921
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| Activity |
IC50 = 64000 nM
|
[1] | |||
| Compound Name |
Chembl4164855
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Investigative | Compound Info | ||
| Synonyms |
BDBM50366285
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| Activity |
IC50 = 80000 nM
|
[2] | |||
| Compound Name |
7-(Cyclopropylamino)-5-pyrrolidin-1-ylpyrazolo[1,5-a]pyrimidine-3-carbonitrile
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4062907
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| Activity |
IC50 ~ 99000 nM
|
[1] | |||
| Compound Name |
7-(Cyclopropylamino)pyrazolo[1,5-a]pyrimidine-3-carbonitrile
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4092313
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| Activity |
IC50 ~ 99000 nM
|
[1] | |||
| Compound Name |
7-Anilino-5-pyrrolidin-1-ylpyrazolo[1,5-a]pyrimidine-3-carbonitrile
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4064121
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| Activity |
IC50 ~ 100000 nM
|
[1] | |||
| Compound Name |
Chembl4169363
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|
Investigative | Compound Info | ||
| Synonyms |
BDBM50366286
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| Activity |
IC50 = 112000 nM
|
[2] | |||
| Compound Name |
Chembl4172762
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Investigative | Compound Info | ||
| Synonyms |
BDBM50366282; F8J
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| Activity |
IC50 = 142000 nM
|
[2] | |||
| Compound Name |
Chembl4176136
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|
Investigative | Compound Info | ||
| Synonyms |
BDBM50366281
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| Activity |
IC50 = 170000 nM
|
[2] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 2 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
2-((5Z)-5-(5-Bromo-2-oxo-1H-indol-3-ylidene)-4-oxo-2-sulfanylidene-1,3-thiazolidin-3-yl)butanedioic acid
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Investigative | Compound Info | ||
| Synonyms |
CID5721353; BCL6 Inhibitor; CHEMBL4066375; 79-6 (CID5721353, BCL6 inhibitor); Oprea1_558002; Oprea1_582624; SCHEMBL10001244; SCHEMBL18586231; BCL6 inhibitor(CID5721353); BCP18443; EX-A1155; BDBM50260534; s8250; STK926357; AKOS000531744; AKOS016037607; AKOS032960253; CCG-269307; MCULE-9483190247; CID-5721353; BS-16815; ST078159; HY-100502; CS-0019629
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| Activity |
IC50 = 212000 nM
|
[3] | |||
| Compound Name |
2-[(4Z)-4-(5-Bromo-2-oxo-1H-indol-3-ylidene)-2-sulfanylidene-1,3-thiazolidin-3-yl]butanedioic acid
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL4069658; BDBM50247637
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| Activity |
IC50 = 212000 nM
|
[4] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Discovery of Pyrazolo[1,5-a]pyrimidine B-Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors. J Med Chem. 2017 May 25;60(10):4386-4402. | ||||
| REF 2 | Identification of Thiourea-Based Inhibitors of the B-Cell Lymphoma 6 BTB Domain via NMR-Based Fragment Screening and Computer-Aided Drug Design. J Med Chem. 2018 Sep 13;61(17):7573-7588. | ||||
| REF 3 | Discovery of a novel B-cell lymphoma 6 (BCL6)-corepressor interaction inhibitor by utilizing structure-based drug design. Bioorg Med Chem. 2017 Sep 1;25(17):4876-4886. | ||||
| REF 4 | X-ray Structures of Target-Ligand Complexes Containing Compounds with Assay Interference Potential. J Med Chem. 2018 Feb 8;61(3):1276-1284. | ||||
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