Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T58589 | Target Info | |||
| Target Name | B1 bradykinin receptor (BDKRB1) | ||||
| Synonyms |
BRADYB1; BK-1 receptor; B1R
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| Target Type | Clinical trial Target | ||||
| Gene Name | BDKRB1 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 4 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
(R)-N-((R)-7-(Hydroxymethyl)chroman-4-yl)-3-(naphthalene-3-sulfonamido)-3-phenylpropanamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL228028; BDBM50209729
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| Activity |
Ki ~ 50000 nM
|
[1] | |||
| Compound Name |
Methyl 2-[4-[[[(2S)-2-(3,3,3-trifluoropropanoylamino)propanoyl]amino]methyl]phenyl]benzoate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL383794; BDBM50182461; methyl 4''-({[N-(3,3,3-trifluoropropanoyl)-L-alanyl]amino}methyl)biphenyl-2-carboxylate
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| Activity |
Ki ~ 50000 nM
|
[2] | |||
| Compound Name |
Methyl 2-[4-[[[2-(3,3,3-trifluoropropanoylamino)acetyl]amino]methyl]phenyl]benzoate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL202463; BDBM50182457; methyl 4''-[({[(3,3,3-trifluoropropanoyl)amino]acetyl}amino)methyl]-1,1''-biphenyl-2-carboxylate
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| Activity |
Ki = 52000 nM
|
[2] | |||
| Compound Name |
N-((R)-6-((Tert-butylamino)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)-2-((S)-1-(1-methyl-1H-imidazol-4-ylsulfonyl)piperidin-2-yl)acetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL206246; BDBM50182244
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Non Binders of This Target (in total, 1 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
(R)-3-(Naphthalene-7-sulfonamido)-3-phenyl-N-((S)-5-(piperidin-1-ylmethyl)-2,3-dihydro-1H-inden-1-yl)propanamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL414091; SCHEMBL4150895; BDBM50203198
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| Activity |
Ki = 241327 nM
|
[4] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Potent nonpeptide antagonists of the bradykinin B1 receptor: structure-activity relationship studies with novel diaminochroman carboxamides. J Med Chem. 2007 May 3;50(9):2200-12. | ||||
| REF 2 | Cyclopropylamino acid amide as a pharmacophoric replacement for 2,3-diaminopyridine. Application to the design of novel bradykinin B1 receptor antagonists. J Med Chem. 2006 Feb 23;49(4):1231-4. | ||||
| REF 3 | A new class of bradykinin 1 receptor antagonists containing the piperidine acetic acid tetralin core. Bioorg Med Chem Lett. 2006 Apr 15;16(8):2071-5. | ||||
| REF 4 | Identification of a nonpeptidic and conformationally restricted bradykinin B1 receptor antagonist with anti-inflammatory activity. J Med Chem. 2007 Feb 22;50(4):607-10. | ||||
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