icatibant   

GtoPdb Ligand ID: 667

Synonyms: D-Arg-[Hyp3,Thi5,D-Tic7,Oic8]BK | Firazyr® | HOE 140 | HOE140
icatibant is an approved drug (EMA (2008), FDA (2011))
Comment: Synthetic analogue of bradykinin. There is some ambiguity in the literature and on online resources as to the exact chemical structure and stereochemistry of icatibant. Therefore, we have chosen not to include a chemical structure here. Users should note that there may not be agreement in the structures represented in the external links provided above.
Selectivity at GPCRs
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Target Sp. Type Action Value Parameter Concentration range (M) Reference
B2 receptor Hs Antagonist Antagonist 8.4 pA2 - 6
pA2 8.4 [6]
B2 receptor Hs Antagonist Antagonist 10.2 pKi - 1
pKi 10.2 (Ki 6.4x10-11 M) [1]
B2 receptor Rn Antagonist Antagonist 10.0 – 10.3 pKi - 4
pKi 10.0 – 10.3 [4]
B2 receptor Mm Antagonist Antagonist 9.6 pKi - 7
pKi 9.6 [7]
B1 receptor Hs Antagonist Antagonist 6.4 – 7.0 pKi - 3,8
pKi 6.4 – 7.0 [3,8]
B1 receptor Rn Antagonist Antagonist 6.1 – 6.4 pKi - 8
pKi 6.1 – 6.4 [8]
B2 receptor Hs Antagonist Antagonist 8.0 – 9.4 pIC50 - 2,7
pIC50 8.0 – 9.4 [2,7]
Ligand mentioned in the following text fields