General Information of the Protein
Protein ID
PT02392
Protein Name
B2 bradykinin receptor
Gene Name
BDKRB2
Secondarily
Gene Name
BKR2
Sequence
MFSPWKISMFLSVREDSVPTTASFSADMLNVTLQGPTLNGTFAQSKCPQVEWLGWLNTIQPPFLWVLFVLATLENIFVLSVFCLHKSSCTVAEIYLGNLAAADLILACGLPFWAITISNNFDWLFGETLCRVVNAIISMNLYSSICFLMLVSIDRYLALVKTMSMGRMRGVRWAKLYSLVIWGCTLLLSSPMLVFRTMKEYSDEGHNVTACVISYPSLIWEVFTNMLLNVVGFLLPLSVITFCTMQIMQVLRNNEMQKFKEIQTERRATVLVLVVLLLFIICWLPFQISTFLDTLHRLGILSSCQDERIIDVITQIASFMAYSNSCLNPLVYVIVGKRFRKKSWEVYQGVCQKGGCRSEPIQMENSMGTLRTSISVERQIHKLQDWAGSRQ
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Peptide receptor (family A GPCR)
>
Short peptide receptor (family A GPCR)
>
Bradykinin receptor
Function
Receptor for bradykinin. It is associated with G proteins that activate a phosphatidylinositol-calcium second messenger system.
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Uniprot ID
P30411
Ensembl ID
ENSG00000168398
HGNC ID
HGNC:1030
Subcellular Location
Cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000052 , A-431
Compound ID Compound Name Compound Formula
CP0847066
4-{(E)-2-[({[2,4-Dichloro-3-(2-methyl-quinolin-8-yloxymethyl)-phenyl]-methyl-carbamoyl}-methyl)-carbamoyl]-vinyl}-N-methyl-benzamide hydrochloride
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C31H29Cl3N4O4
 1
1
IC50 = 1.3 nM
   TI
   LI
   LO
   TS
CP0943579
4-{(E)-2-[({[3-(3-Bromo-2-methyl-imidazo[1,2-a]pyridin-8-yloxymethyl)-2,4-dichloro-phenyl]-methyl-carbamoyl}-methyl)-carbamoyl]-vinyl}-N,N-dimethyl-benzamide hydrochloride
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C30H29BrCl3N5O4
 1
1
IC50 = 1.4 nM
   TI
   LI
   LO
   TS
CP0885378
4-{(E)-2-[({[3-(3-Bromo-2-methyl-imidazo[1,2-a]pyridin-8-yloxymethyl)-2,4-dichloro-phenyl]-methyl-carbamoyl}-methyl)-carbamoyl]-vinyl}-N-methyl-benzamide hydrochloride
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C29H27BrCl3N5O4
 1
1
IC50 = 1.5 nM
   TI
   LI
   LO
   TS
CP0945053
(E)-3-(4-Acetylamino-phenyl)-N-({[3-(3-bromo-2-methyl-imidazo[1,2-a]pyridin-8-yloxymethyl)-2,4-dichloro-phenyl]-methyl-carbamoyl}-methyl)-acrylamide hydrochloride
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C29H27BrCl3N5O4
 1
1
IC50 = 1.6 nM
   TI
   LI
   LO
   TS
CP0887793
3-(6-Acetylamino-pyridin-3-yl)-N-({[3-(3-bromo-2-methyl-imidazo[1,2-a]pyridin-8-yloxymethyl)-2,4-dichloro-phenyl]-methyl-carbamoyl}-methyl)-acrylamide; Dihydrochloride
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C28H27BrCl4N6O4
 1
1
IC50 = 2.4 nM
   TI
   LI
   LO
   TS
CP0885577
(E)-N-({[3-(3-Bromo-2-methyl-imidazo[1,2-a]pyridin-8-yloxymethyl)-2,4-dichloro-phenyl]-methyl-carbamoyl}-methyl)-3-[4-(3-methyl-ureido)-phenyl]-acrylamide hydrochloride
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C29H28BrCl3N6O4
 1
1
IC50 = 2.6 nM
   TI
   LI
   LO
   TS
CP0885377
4-{(E)-2-[({[2,4-Dichloro-3-(3-methyl-quinoxalin-5-yloxymethyl)-phenyl]-methyl-carbamoyl}-methyl)-carbamoyl]-vinyl}-N-methyl-benzamide hydrochloride
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C30H28Cl3N5O4
 1
1
IC50 = 3.1 nM
   TI
   LI
   LO
   TS
CP0404246
Firazyr
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C59H89N19O13S
 1
1
IC50 = 3.3 nM
   TI
   LI
   LO
   TS
CP0885966
5-{2-[({[3-(3-Bromo-2-methyl-imidazo[1,2-a]pyridin-8-yloxymethyl)-2,4-dichloro-phenyl]-methyl-carbamoyl}-methyl)-carbamoyl]-vinyl}-pyridine-2-carboxylic acid dimethylamide; Dihydrochloride
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C29H29BrCl4N6O4
 1
1
IC50 = 3.7 nM
   TI
   LI
   LO
   TS
CP0902615
(E)-N-({[3-(3-Bromo-2-methyl-imidazo[1,2-a]pyridin-8-yloxymethyl)-2,4-dichloro-phenyl]-methyl-carbamoyl}-methyl)-3-[4-(2-oxo-pyrrolidin-1-yl)-phenyl]-acrylamide hydrochloride
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C31H29BrCl3N5O4
 1
1
IC50 = 4.1 nM
   TI
   LI
   LO
   TS
CP0902447
(E)-N-({[3-(3-Bromo-2-methyl-imidazo[1,2-a]pyridin-8-yloxymethyl)-2,4-dichloro-phenyl]-methyl-carbamoyl}-methyl)-3-(4-methanesulfonylamino-phenyl)-acrylamide hydrochloride
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C28H27BrCl3N5O5S
 1
1
IC50 = 4.8 nM
   TI
   LI
   LO
   TS
CP0885937
5-{2-[({[3-(3-Bromo-2-methyl-imidazo[1,2-a]pyridin-8-yloxymethyl)-2,4-dichloro-phenyl]-methyl-carbamoyl}-methyl)-carbamoyl]-vinyl}-pyridine-2-carboxylic acid methylamide; Dihydrochloride
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C28H27BrCl4N6O4
 1
1
IC50 = 9.1 nM
   TI
   LI
   LO
   TS
CP0457306
3-{(E)-2-[({[2,4-Dichloro-3-(2-methyl-quinolin-8-yloxymethyl)-phenyl]-methyl-carbamoyl}-methyl)-carbamoyl]-vinyl}-N,N-dimethyl-benzamide
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C32H30Cl2N4O4
 1
1
IC50 = 14 nM
   TI
   LI
   LO
   TS
CP0943624
(E)-3-[4-(Acetyl-methyl-amino)-phenyl]-N-({[3-(3-bromo-2-methyl-imidazo[1,2-a]pyridin-8-yloxymethyl)-2,4-dichloro-phenyl]-methyl-carbamoyl}-methyl)-acrylamide hydrochloride
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C30H29BrCl3N5O4
 1
1
IC50 = 16 nM
   TI
   LI
   LO
   TS
CP0882976
3-[3-({[3-(3-Bromo-2-methyl-imidazo[1,2-a]pyridin-8-yloxymethyl)-2,4-dichloro-phenyl]-methyl-carbamoyl}-methyl)-ureido]-N-(2-methoxy-ethyl)-benzamide hydrochloride
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C29H30BrCl3N6O5
 1
1
IC50 = 20 nM
   TI
   LI
   LO
   TS
CP0920265
3-[3-({[3-(3-Bromo-2-methyl-imidazo[1,2-a]pyridin-8-yloxymethyl)-2,4-dichloro-phenyl]-methyl-carbamoyl}-methyl)-ureido]-N,N-dimethyl-benzamide hydrochloride
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C28H28BrCl3N6O4
 1
1
IC50 = 20 nM
   TI
   LI
   LO
   TS
CP0392560
4-{(E)-2-[({[2,4-Dichloro-3-(1,2-dimethyl-1H-benzoimidazol-4-yloxymethyl)-phenyl]-methyl-carbamoyl}-methyl)-carbamoyl]-vinyl}-N-methyl-benzamide
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C30H29Cl2N5O4
 1
1
IC50 = 43 nM
   TI
   LI
   LO
   TS
CP0465050
4-{(E)-2-[({[2,4-Dichloro-3-(2-methyl-quinazolin-8-yloxymethyl)-phenyl]-methyl-carbamoyl}-methyl)-carbamoyl]-vinyl}-N-methyl-benzamide
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C30H27Cl2N5O4
 1
1
IC50 = 59 nM
   TI
   LI
   LO
   TS
CP0902432
2-[3-(3-Acetyl-phenyl)-ureido]-N-[3-(3-bromo-2-methyl-imidazo[1,2-a]pyridin-8-yloxymethyl)-2,4-dichloro-phenyl]-N-methyl-acetamide hydrochloride
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C27H25BrCl3N5O4
 1
1
IC50 = 61 nM
   TI
   LI
   LO
   TS
CP0395223
N-[3-[(3-bromo-2-methylimidazo[1,2-a]pyridin-8-yl)oxymethyl]-2,4-dichlorophenyl]-2-[[3-[(2-methoxyacetyl)amino]phenyl]carbamoylamino]-N-methylacetamide
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C28H27BrCl2N6O5
 1
1
IC50 = 75 nM
   TI
   LI
   LO
   TS
CP0897038
(Z)-N-({[3-(3-Bromo-2-methyl-imidazo[1,2-a]pyridin-8-yloxymethyl)-2,4-dichloro-phenyl]-methyl-carbamoyl}-methyl)-3-phenyl-acrylamide hydrochloride
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C27H24BrCl3N4O3
 1
1
IC50 = 120 nM
   TI
   LI
   LO
   TS
CP0946107
N-[3-(3-Bromo-2-methyl-imidazo[1,2-a]pyridin-8-yloxymethyl)-2,4-dichloro-phenyl]-N-methyl-2-(3-m-tolyl-ureido)-acetamide hydrochloride
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C26H25BrCl3N5O3
 1
1
IC50 = 140 nM
   TI
   LI
   LO
   TS
CP0470615
N-[3-[(3-bromo-2-methylimidazo[1,2-a]pyridin-8-yl)oxymethyl]-2,4-dichlorophenyl]-N-methyl-2-[(2-methylphenyl)carbamoylamino]acetamide
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C26H24BrCl2N5O3
 1
1
IC50 = 150 nM
   TI
   LI
   LO
   TS
CP0523171
3-[3-({[3-(3-Bromo-2-methyl-imidazo[1,2-a]pyridin-8-yloxymethyl)-2,4-dichloro-phenyl]-methyl-carbamoyl}-methyl)-ureido]-benzoic acid ethyl ester
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C28H26BrCl2N5O5
 1
1
IC50 = 150 nM
   TI
   LI
   LO
   TS
CP0902621
N-[3-(3-Bromo-2-methyl-imidazo[1,2-a]pyridin-8-yloxymethyl)-2,4-dichloro-phenyl]-N-methyl-2-(3-phenyl-ureido)-acetamide hydrochloride
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C25H23BrCl3N5O3
 1
1
IC50 = 150 nM
   TI
   LI
   LO
   TS
CP0856319
N-[3-(3-Bromo-2-methyl-imidazo[1,2-a]pyridin-8-yloxymethyl)-2,4-dichloro-phenyl]-N-methyl-2-[3-(3-nitro-phenyl)-ureido]-acetamide hydrochloride
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C25H22BrCl3N6O5
 1
1
IC50 = 180 nM
   TI
   LI
   LO
   TS
CP0895135
N-[3-(3-Bromo-2-methyl-imidazo[1,2-a]pyridin-8-yloxymethyl)-2,4-dichloro-phenyl]-2-[3-(3-cyano-phenyl)-ureido]-N-methyl-acetamide hydrochloride
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C26H22BrCl3N6O3
 1
1
IC50 = 190 nM
   TI
   LI
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CP0861119
N-[3-(3-Bromo-2-methyl-imidazo[1,2-a]pyridin-8-yloxymethyl)-2,4-dichloro-phenyl]-2-[3-(3-methoxy-phenyl)-ureido]-N-methyl-acetamide hydrochloride
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C26H25BrCl3N5O4
 1
1
IC50 = 200 nM
   TI
   LI
   LO
   TS
CP0463789
N-[2-[3-[(3-bromo-2-methylimidazo[1,2-a]pyridin-8-yl)oxymethyl]-2,4-dichloro-N-methylanilino]-2-oxoethyl]hexanamide
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C24H27BrCl2N4O3
 1
1
IC50 = 240 nM
   TI
   LI
   LO
   TS
CP0885625
N-[3-(3-Bromo-2-methyl-imidazo[1,2-a]pyridin-8-yloxymethyl)-2,4-dichloro-phenyl]-N-methyl-2-(3-p-tolyl-ureido)-acetamide hydrochloride
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C26H25BrCl3N5O3
 1
1
IC50 = 260 nM
   TI
   LI
   LO
   TS
CP0535264
N-[2-[3-[(3-bromo-2-methylimidazo[1,2-a]pyridin-8-yl)oxymethyl]-2,4-dichloro-N-methylanilino]-2-oxoethyl]-3-phenylpropanamide
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C27H25BrCl2N4O3
 1
1
IC50 = 350 nM
   TI
   LI
   LO
   TS
CP0445309
N-[2-[3-[(3-bromo-2-methylimidazo[1,2-a]pyridin-8-yl)oxymethyl]-2,4-dichloro-N-methylanilino]-2-oxoethyl]-4-phenylbutanamide
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C28H27BrCl2N4O3
 1
1
IC50 = 480 nM
   TI
   LI
   LO
   TS
CP0374222
N-[3-[(3-bromo-2-methylimidazo[1,2-a]pyridin-8-yl)oxymethyl]-2,4-dichlorophenyl]-N-methyl-2-[(2-phenoxyacetyl)amino]acetamide
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C26H23BrCl2N4O4
 1
1
IC50 = 510 nM
   TI
   LI
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   TS
CP0410477
2-(3-Benzoyl-ureido)-N-[3-(3-bromo-2-methyl-imidazo[1,2-a]pyridin-8-yloxymethyl)-2,4-dichloro-phenyl]-N-methyl-acetamide
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C26H22BrCl2N5O4
 1
1
IC50 = 510 nM
   TI
   LI
   LO
   TS
CP0885968
2-(3-Benzyl-ureido)-N-[3-(3-bromo-2-methyl-imidazo[1,2-a]pyridin-8-yloxymethyl)-2,4-dichloro-phenyl]-N-methyl-acetamide hydrochloride
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C26H25BrCl3N5O3
 1
1
IC50 = 570 nM
   TI
   LI
   LO
   TS
CP0454516
N-[2-[3-[(3-bromo-2-methylimidazo[1,2-a]pyridin-8-yl)oxymethyl]-2,4-dichloro-N-methylanilino]-2-oxoethyl]butanamide
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C22H23BrCl2N4O3
 1
1
IC50 = 610 nM
   TI
   LI
   LO
   TS
CP0885535
N-({[3-(3-Bromo-2-methyl-imidazo[1,2-a]pyridin-8-yloxymethyl)-2,4-dichloro-phenyl]-methyl-carbamoyl}-methyl)-2-phenyl-acetamide hydrochloride
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C26H24BrCl3N4O3
 1
1
IC50 = 670 nM
   TI
   LI
   LO
   TS
CP0429345
N-[3-[(3-bromo-2-methylimidazo[1,2-a]pyridin-8-yl)oxymethyl]-2,4-dichlorophenyl]-2-[[2-(dimethylamino)acetyl]amino]-N-methylacetamide
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C22H24BrCl2N5O3
 1
1
IC50 = 830 nM
   TI
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   TS
CP0494786
4-{(E)-2-[({[2,4-Dichloro-3-(2-methyl-benzooxazol-4-yloxymethyl)-phenyl]-methyl-carbamoyl}-methyl)-carbamoyl]-vinyl}-N-methyl-benzamide
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C29H26Cl2N4O5
 1
1
IC50 = 860 nM
   TI
   LI
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   TS
CP0891122
N-[3-(3-Bromo-2-methyl-imidazo[1,2-a]pyridin-8-yloxymethyl)-2,4-dichloro-phenyl]-2-[3-(3-chloro-phenyl)-ureido]-N-methyl-acetamide hydrochloride
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C25H22BrCl4N5O3
 1
1
IC50 = 1900 nM
   TI
   LI
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   TS
CP0511366
N-[3-[(3-bromo-2-methylimidazo[1,2-a]pyridin-8-yl)oxymethyl]-2,4-dichlorophenyl]-2-(ethylcarbamoylamino)-N-methylacetamide
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C21H22BrCl2N5O3
 1
1
IC50 = 3000 nM
   TI
   LI
   LO
   TS
CP0511276
4-((E)-2-{[({2,4-Dichloro-3-[2-(2,5-dimethyl-pyrrol-1-yl)-pyridin-3-yloxymethyl]-phenyl}-methyl-carbamoyl)-methyl]-carbamoyl}-vinyl)-N-methyl-benzamide
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C32H31Cl2N5O4
 1
1
IC50 = 3500 nM
   TI
   LI
   LO
   TS
CP0920729
2-Acetylamino-N-[3-(3-bromo-2-methyl-imidazo[1,2-a]pyridin-8-yloxymethyl)-2,4-dichloro-phenyl]-N-methyl-acetamide hydrochloride
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C20H20BrCl3N4O3
 1
1
IC50 = 4100 nM
   TI
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   LO
   TS
CP0383199
4-{(E)-2-[({[2,4-Dichloro-3-(2-methyl-quinoxalin-5-yloxymethyl)-phenyl]-methyl-carbamoyl}-methyl)-carbamoyl]-vinyl}-N-methyl-benzamide
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C30H27Cl2N5O4
 1
1
IC50 = 4300 nM
   TI
   LI
   LO
   TS
CP0410512
3-[3-({[3-(3-Bromo-2-methyl-imidazo[1,2-a]pyridin-8-yloxymethyl)-2,4-dichloro-phenyl]-methyl-carbamoyl}-methyl)-ureido]-benzoic acid
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C26H22BrCl2N5O5
 1
1
IC50 = 5200 nM
   TI
   LI
   LO
   TS
CP0377942
4-{(E)-2-[({[2,4-Dichloro-3-(6-methyl-pyridin-2-ylmethoxymethyl)-phenyl]-methyl-carbamoyl}-methyl)-carbamoyl]-vinyl}-N-methyl-benzamide
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C28H28Cl2N4O4
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0410682
4-{(E)-2-[({[2,4-Dichloro-3-(3-methyl-isoquinolin-5-yloxymethyl)-phenyl]-methyl-carbamoyl}-methyl)-carbamoyl]-vinyl}-N-methyl-benzamide
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C31H28Cl2N4O4
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0521181
4-{(E)-2-[({[2,4-Dichloro-3-(2-methyl-quinolin-7-yloxymethyl)-phenyl]-methyl-carbamoyl}-methyl)-carbamoyl]-vinyl}-N-methyl-benzamide
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C31H28Cl2N4O4
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0394067
2-[3-(3-Amino-phenyl)-ureido]-N-[3-(3-bromo-2-methyl-imidazo[1,2-a]pyridin-8-yloxymethyl)-2,4-dichloro-phenyl]-N-methyl-acetamide
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C25H23BrCl2N6O3
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0256063
(E)-N-[2-[2,4-dichloro-N-methyl-3-[[2-methyl-4-(pyridin-2-ylmethoxy)quinolin-8-yl]oxymethyl]anilino]-2-oxoethyl]-3-[6-[(E)-2-pyridin-4-ylethenyl]pyridin-3-yl]prop-2-enamide
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C41H34Cl2N6O4
 1
1 IC50 = 0.36 nM
CP0304790
4-((E)-2-{[({2,4-Dichloro-3-[2-methyl-4-(pyridin-2-ylmethoxy)-quinolin-8-yloxymethyl]-phenyl}-methyl-carbamoyl)-methyl]-carbamoyl}-vinyl)-N-methyl-benzamide
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C37H33Cl2N5O5
 1
1 IC50 = 0.41 nM
CP0335342
(E)-3-(6-Acetylamino-pyridin-3-yl)-N-({[2,4-dichloro-3-(2-methoxy-1-pyridin-2-ylmethyl-1H-benzoimidazol-4-yloxymethyl)-phenyl]-methyl-carbamoyl}-methyl)-acrylamide
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C34H31Cl2N7O5
 1
1 IC50 = 0.69 nM
CP0128813
(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S,4R)-1-[(2S)-1-[(2S)-2-[[(2R)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]-4-hydroxypyrrolidine-2-carbonyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoic acid
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C60H87N19O13
 3
1 IC50 = 7 nM
2 IC50 = 10 nM
3 IC50 = 14 nM
CP0309352
8-[3-chloro-5-(thiazol-2-ylsulfanyl)-pyridin-4-ylmethoxy]-2-methyl-4-(2-methyl-2Hpyrazol-3-yl)-quinoline
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C23H18ClN5OS2
 1
1 IC50 = 470 nM
CP0299612
(BK) H-Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg-OH
   Show/Hide
C50H73N15O11
 1
1 Ki = 0.11 nM
Clinical Information about the Protein
Target 1 ( B2 bradykinin receptor (BDKRB2) )
Target Type Successful Target
Disease 5 Target-related Diseases  5
1 Hereditary angioedema [ICD-11: 4A00.14]
2 Osteoarthritis [ICD-11: FA00-FA05]
3 Brain cancer [ICD-11: 2A00]
4 Rhinitis [ICD-11: FA20]
5 Pain [ICD-11: MG30-MG3Z]
Approved Drug(s) 1 Approved Drug  1
1 Icatibant Approved
Hereditary angioedema
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 Fasitibant chloride Phase 2
Osteoarthritis
Discontinued Drug(s) 3 Discontinued Drugs  3
1 Labradimil Discontinued in Phase 2
Brain cancer
2 NPC-567 Discontinued in Phase 2
Rhinitis
3 JSM-10292 Terminated
Pain
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT07055 B2 bradykinin receptor Rattus norvegicus, Rat