CAS_58-82-2 NSC_105044 Bradykinin BDBM82076
Galanin-(1-13)-bradykinin-(2-9)-amide Galanin (1-13)-bradikinin(2-9) CHEMBL503473 BDBM50273370 GWTLNSAGYLLGPPPGFSPFR-CONH2 M35
(bradykinin triacetate)2-(2-{[1-(2-{2-[2-({1-[1-(2-Amino-5-guanidino-pentanoyl)-pyrrolidine-2-carbonyl]-pyrrolidine-2-carbonyl}-amino)-acetylamino]-3-phenyl-propionylamino}-3-hydroxy-propionyl)-pyrrolidine-2-carbonyl]-amino}-3-phenyl-propionylamino)-5-guanidino-pentanoic acid (BK) H-Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg-OH CHEMBL406291 bradykinin BDBM50049949 2-(2-{[1-(2-{2-[2-({1-[1-(2-Amino-5-guanidino-pentanoyl)-pyrrolidine-2-carbonyl]-pyrrolidine-2-carbonyl}-amino)-acetylamino]-3-phenyl-propionylamino}-3-hydroxy-propionyl)-pyrrolidine-2-carbonyl]-amino}-3-phenyl-propionylamino)-5-guanidino-pentanoic acid 2-(2-{[1-(2-{2-[2-({1-[1-(2-Amino-5-guanidino-pentanoyl)-pyrrolidine-2-carbonyl]-pyrrolidine-2-carbonyl}-amino)-acetylamino]-3-phenyl-propionylamino}-3-hydroxy-propionyl)-pyrrolidine-2-carbonyl]-amino}-3-phenyl-propionylamino)-5-guanidino-pentanoic acid(Bradykinin)
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- Sawada, Y; Kayakiri, H; Abe, Y; Imai, K; Mizutani, T; Inamura, N; Asano, M; Aramori, I; Hatori, C; Katayama, A; Oku, T; Tanaka, H A new series of highly potent non-peptide bradykinin B2 receptor antagonists incorporating the 4-heteroarylquinoline framework. Improvement of aqueous solubility and new insights into species difference. J Med Chem 47: 1617-30 (2004)
- Sawada, Y; Kayakiri, H; Abe, Y; Mizutani, T; Inamura, N; Asano, M; Aramori, I; Hatori, C; Oku, T; Tanaka, H A new class of nonpeptide bradykinin B(2) receptor ligand, incorporating a 4-aminoquinoline framework. Identification of a key pharmacophore to determine species difference and agonist/antagonist profile. J Med Chem 47: 2667-77 (2004)
- ChEMBL_40276 (CHEMBL653409) Binding affinity towards bradykinin receptor B2 using [3H]bradykinin
- ChEMBL_1559755 (CHEMBL3779535) Displacement of [3H]bradykinin from human recombinant B2 bradykinin receptor
- ChEBML_40423 Binding affinity against human bradykinin receptor B2 using [3H]bradykinin as radioligand
- ChEMBL_40423 (CHEMBL652638) Binding affinity against human bradykinin receptor B2 using [3H]bradykinin as radioligand
- ChEMBL_429986 (CHEMBL917716) Displacement of [3H]bradykinin from human bradykinin B2 receptor expressed in CHO cells
- ChEBML_40275 Binding affinity against [3H]bradykinin binding to bradykinin receptor B2 in guinea pig ileal membrane
- ChEMBL_425212 (CHEMBL855158) Displacement of [3H]bradykinin from human bradykinin B2 receptor expressed in CHO-K1 cells
- ChEMBL_643606 (CHEMBL1212470) Displacement of [3H]bradykinin from human recombinant bradykinin B2 receptor expressed in CHO cells
- ChEMBL_806223 (CHEMBL1958764) Displacement of [3H][desArg9]Lys-Bradykinin from human bradykinin B1 receptor expressed in CHO cells
- ChEMBL_40426 (CHEMBL652641) Binding affinity towards human cloned Bradykinin receptor B2 expressed in CHO cells by [3H]bradykinin displacement.
- ChEMBL_40441 (CHEMBL652380) Binding affinity against rat Bradykinin receptor B2 expressed in CHO cells using [3H]-bradykinin as radioligand
- ChEMBL_40442 (CHEMBL652381) Binding affinity against rat bradykinin B2 receptors expressed in CHO cells using [3H]bradykinin as radioligand
- ChEMBL_40130 (CHEMBL658496) Binding affinity against human cloned Bradykinin receptor B1 expressed in CHO cells using [3H]-bradykinin as radioligand
- ChEMBL_40422 (CHEMBL652637) Binding affinity against human cloned Bradykinin receptor B2 expressed in CHO cells using [3H]-bradykinin as radioligand
- ChEMBL_965476 (CHEMBL2395280) Displacement of [3H]Bradykinin from human recombinant bradykinin B2 receptor expressed in CHEM1 cells after 60 mins
- Binding Assay Binding assay using Bradykinin-1 receptor.
- ChEBML_40424 Binding affinity towards human bradykinin receptor B2
- ChEMBL_333385 (CHEMBL859129) Binding affinity to bradykinin B2 receptor
- ChEMBL_39982 (CHEMBL653556) Inhibition of human bradykinin B1 receptor
- ChEMBL_423710 (CHEMBL913022) Inhibition of human bradykinin B2 receptor
- ChEMBL_535289 (CHEMBL982614) Inhibition of human bradykinin B1 receptor
- ChEMBL_662793 (CHEMBL1252532) Inhibition of rabbit bradykinin B1 receptor
- ChEMBL_662794 (CHEMBL1252533) Inhibition of rat bradykinin B1 receptor
- ChEMBL_879298 (CHEMBL2208696) Antagonist activity at Bradykinin B1 receptor
- ChEMBL_497315 (CHEMBL995877) Displacement of [3H]Lys-bradykinin from human recombinant bradykinin B1 receptor expressed in CHO cells by scintillation counting
- ChEBML_40429 In vitro binding affinity against Bradykinin receptor B2
- ChEMBL_2297250 Binding affinity to B2 bradykinin receptor (unknown origin)
- ChEMBL_302466 (CHEMBL826332) Binding affinity against Human bradykinin receptor B1
- ChEMBL_423681 (CHEMBL853755) Binding affinity to rat bradykinin B1 receptor
- ChEMBL_423682 (CHEMBL853760) Binding affinity to rabbit bradykinin B1 receptor
- ChEMBL_429982 (CHEMBL917712) Binding affinity to rabbit bradykinin B1 receptor
- ChEMBL_434373 (CHEMBL919421) Antagonist activity at rat bradykinin B1 receptor
- ChEMBL_434374 (CHEMBL919418) Antagonist activity at rabbit bradykinin B1 receptor
- ChEMBL_443978 (CHEMBL893140) Binding affinity at human bradykinin B1 receptor
- ChEMBL_487377 (CHEMBL1021904) Binding affinity to human bradykinin B1 receptor
- ChEMBL_535281 (CHEMBL982606) Antagonist activity at rat bradykinin B1 receptor
- ChEMBL_662796 (CHEMBL1252535) Binding affinity to human bradykinin B1 receptor
- ChEMBL_662797 (CHEMBL1252536) Antagonist activity at dog bradykinin B1 receptor
- ChEMBL_662798 (CHEMBL1252537) Binding affinity to rat bradykinin B1 receptor
- ChEMBL_662799 (CHEMBL1252538) Binding affinity to mouse bradykinin B1 receptor
- ChEMBL_662800 (CHEMBL1252539) Binding affinity to monkey bradykinin B1 receptor
- ChEMBL_748611 (CHEMBL1780464) Antagonist activity at human bradykinin B1 receptor
- ChEMBL_796433 (CHEMBL1937748) Binding affinity to human B1 bradykinin receptor
- ChEMBL_814368 (CHEMBL2019577) Binding affinity to human bradykinin B1 receptor
- ChEMBL_814371 (CHEMBL2019580) Antagonist activity at rat bradykinin B1 receptor
- ChEMBL_610511 (CHEMBL1064982) Antagonist activity at bradykinin B1 receptor in human IMR90 cells assessed as inhibition of des-Arg-bradykinin-mediated calcium mobilization
- ChEMBL_612385 (CHEMBL1066271) Antagonist activity at bradykinin B1 receptor in human IMR90 cells assessed as inhibition of des-Arg-bradykinin-mediated calcium mobilization
- ChEMBL_806221 (CHEMBL1958762) Displacement of [3H]-Bradykinin from human bradykinin B2 receptor expressed in CHO cells membrane after 60 mins by scintillation counting
- ChEMBL_806231 (CHEMBL1958772) Antagonist activity at guinea pig bradykinin B2 receptor in longitudinal smooth muscle assessed as inhibition of bradykinin-induced contractile responses
- ChEMBL_523549 (CHEMBL1001563) Antagonist activity at human recombinant bradykinin 2 receptor expressed in CHO cells assessed as inhibition of bradykinin-induced intracellular calcium mobilization
- Calcium Mobilization Assay Calcium mobilization assay using Bradykinin-1 receptor.
- ChEMBL_2078239 (CHEMBL4734030) Agonist activity at bradykinin B2 receptor (unknown origin)
- ChEMBL_423683 (CHEMBL853765) Binding affinity to rhesus monkey bradykinin B1 receptor
- ChEMBL_658534 (CHEMBL1247736) Binding affinity to human recombinant bradykinin B1 receptor
- ChEMBL_658535 (CHEMBL1247737) Binding affinity to human recombinant bradykinin B2 receptor
- ChEMBL_1633556 (CHEMBL3876348) Displacement of [3H]bradykinin from human recombinant bradykinin B2 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
- ChEMBL_1861205 (CHEMBL4362061) Displacement of [3H]bradykinin from human recombinant bradykinin B2 receptor expressed in CHO cells incubated for 2 hrs by liquid scintillation counter
- ChEMBL_806222 (CHEMBL1958763) Antagonist activity at human bradykinin B2 receptor expressed in dhfr-deficient CHO cells assessed as inhibition of bradykinin-induced inositol monophosphate accumulation preincubated for 15 mins prior bradykinin induction measured after 40 mins by liquid scintillation spectrometry
- ChEMBL_305717 (CHEMBL829390) Inhibition of Bradykinin receptor B1 expressed in HEK293 cells
- ChEMBL_572632 (CHEMBL1026056) Displacement of [3H]bradykinin from wild-type B2 receptor
- ChEMBL_572638 (CHEMBL1026062) Displacement of [3H]bradykinin from guinea pig B2 receptor
- ChEBML_40431 Tested for binding affinity against human IMR-90 Bradykinin receptor B2
- ChEMBL_2023082 (CHEMBL4676895) Displacement of [3H]nicotine from B2 bradykinin receptor (unknown origin)
- ChEMBL_302814 (CHEMBL839504) Binding affinity for Bradykinin receptor B2 expressed in COS7 cells
- ChEMBL_302842 (CHEMBL827887) Binding affinity for Bradykinin receptor B1 expressed in HEK293 cells
- ChEMBL_321573 (CHEMBL881788) Inhibitory concentration against endothelin converting enzyme 1 using bradykinin-derived
- ChEMBL_40138 (CHEMBL876936) Compound was tested for inhibition against rat Bradykinin receptor B1
- ChEMBL_429983 (CHEMBL917713) Activity at rabbit bradykinin B1 receptor assessed by FLIPR assay
- ChEMBL_443979 (CHEMBL893141) Antagonist activity in human bradykinin B1 receptor by FLIPR method
- ChEMBL_463210 (CHEMBL947207) Binding affinity to human bradykinin B1 receptor by FLIPR assay
- ChEBML_40277 In vitro binding affinity against bradykinin receptor B2 from guinea pig ileum.
- ChEBML_40427 Binding affinity against human IMR 90 fetal lung fibroblast bradykinin receptor B2
- ChEMBL_1561510 (CHEMBL3776147) Inhibition of recombinant human bradykinin receptor 2 expressed in CHO cells
- ChEMBL_321543 (CHEMBL881481) Inhibitory concentration against endothelin converting enzyme 1 using bradykinin-derived substrate
- ChEMBL_333384 (CHEMBL859128) Binding affinity to human bradykinin B1 receptor expressed in CHO cells
- ChEMBL_40431 (CHEMBL652645) Tested for binding affinity against human IMR-90 Bradykinin receptor B2
- ChEMBL_463209 (CHEMBL947206) Binding affinity to human bradykinin B1 receptor expressed in CHO cells
- ChEMBL_463211 (CHEMBL947208) Binding affinity to rat bradykinin B1 receptor expressed in CHO cells
- ChEMBL_463212 (CHEMBL947209) Binding affinity to monkey bradykinin B1 receptor expressed in CHO cells
- ChEMBL_463213 (CHEMBL947210) Binding affinity to rabbit bradykinin B1 receptor expressed in CHO cells
- ChEMBL_463214 (CHEMBL947211) Binding affinity to dog bradykinin B1 receptor expressed in CHO cells
- ChEMBL_463823 (CHEMBL948902) Binding affinity to human bradykinin B1 receptor expressed in rat CNS
- ChEMBL_644658 (CHEMBL1211637) Displacement of [3H]Lys-desArg9-BK from human bradykinin B1 receptor
- ChEMBL_796432 (CHEMBL1937747) Antagonist activity at rabbit B1 bradykinin receptor expressed in CHO cells
- ChEMBL_964329 (CHEMBL2395591) Binding affinity to human bradykinin B2 receptor by radioligand displacement assay
- ChEMBL_966197 (CHEMBL2395702) Binding affinity to human bradykinin B2 receptor by radioligand displacement assay
- ChEBML_40106 Binding affinity against human IMR90 fetal lung fibroblast bradykinin B2 receptor was evaluated
- ChEBML_40141 Compound was evaluated for competitive [3H]bradykinin binding to guinea pig ileum homogenates
- ChEMBL_302733 (CHEMBL838681) Binding affinity of the [35S]- radiolabeled compound to dog Bradykinin receptor B1
- ChEMBL_302734 (CHEMBL876354) Binding affinity of the [35S]- radiolabeled compound to rat Bradykinin receptor B1
- ChEMBL_302791 (CHEMBL839475) Binding affinity of the [35S]- radiolabeled compound to rabbit Bradykinin receptor B1
- ChEMBL_40139 (CHEMBL656133) Antagonistic activity against Bradykinin receptor B1 of rat ileum longitudinal smooth muscle.
- ChEMBL_40427 (CHEMBL652642) Binding affinity against human IMR 90 fetal lung fibroblast bradykinin receptor B2
- ChEMBL_40437 (CHEMBL652376) Inhibition of Bradykinin receptor B2-mediated contractions of rat uterus smooth muscle
- ChEMBL_302897 (CHEMBL830212) Binding affinity of the [35S]- radiolabeled compound to rhesus monkey Bradykinin receptor B1
- ChEMBL_302988 (CHEMBL830227) Inhibitory constant against human Bradykinin receptor B1 expressed in chinese hamster ovary cells
- ChEMBL_39981 (CHEMBL653555) Compound was tested for inhibition against human bradykinin B1 receptor using FLIPR assay
- ChEMBL_40135 (CHEMBL656787) In vitro Bradykinin receptor B1 antagonist activity in functional tissue within rabbit aorta
- ChEMBL_40137 (CHEMBL656789) Compound was tested for inhibition against rat Bradykinin receptor B1 using FLIPR assay
- ChEMBL_40279 (CHEMBL653412) Antagonistic activity against Bradykinin receptor B2 of guinea pig ileum longitudinal smooth muscle.
- ChEMBL_40283 (CHEMBL653415) Antagonism of the [Ca2+] efflux actions of human Bradykinin receptor B2 (WI38 fibroblasts)
- ChEMBL_40445 (CHEMBL652384) In vitro Bradykinin receptor B2 antagonist activity by using rat uterus functional assay
- ChEMBL_434360 (CHEMBL919419) Displacement of [3H]DAK from human bradykinin B1 receptor expressed in CHOD cells
- ChEMBL_510232 (CHEMBL1005610) Antagonist activity at human bradykinin B1 receptor expressed in CHO-D-/aequorin cells
- ChEMBL_572637 (CHEMBL1026061) Displacement of [3H]bradykinin from human recombinant B2 receptor expressed in HEK293 cells
- ChEBML_40297 Compound was assayed for binding against the human Bradykinin receptor B2 expressed in CHO cells
- ChEMBL_40271 (CHEMBL656506) In vitro antagonistic activity for Bradykinin receptor B2 by guinea pig pulmonary artery assay.
- ChEMBL_40285 (CHEMBL653417) Antagonism of the [Ca2+] efflux actions of the human Bradykinin receptor B2 (WI38 fibroblasts)
- ChEMBL_425211 (CHEMBL855157) Displacement of [3H]DAK from human bradykinin B1 receptor expressed in CHO-D cells
- ChEBML_1711424 Displacement of [3H]bradykinin from human recombinant B2 receptor after 60 mins by scintillation counting analysis
- ChEMBL_40270 (CHEMBL656505) In vitro antagonistic activity for Bradykinin receptor B2 by guinea pig ileal membrane receptor assay.
- ChEMBL_40282 (CHEMBL653414) Antagonism of the [Ca2+] efflux actions of human Bradykinin receptor B2 (SK-N-SH neuroblastoma)
- ChEMBL_40428 (CHEMBL652643) Ability to bind to human cloned B2 receptor in competition binding experiments with [3H]- bradykinin
- ChEMBL_425214 (CHEMBL855160) Antagonistic activity at rat bradykinin B1 receptor assessed as effect on DAK-mediated calcium mobilization
- ChEMBL_429981 (CHEMBL917711) Displacement of [3H]des-arg10 kallidin from rat bradykinin B1 receptor expressed in CHO cells
- ChEMBL_446485 (CHEMBL895597) Displacement of [3H]DAKA from human bradykinin B1 receptor in IL1-beta stimulated IMR90 cells
- ChEMBL_1861204 (CHEMBL4362060) Displacement of [3H]BK from Bradykinin B2 Receptor in guinea pig ileum by liquid scintillation counter
- ChEMBL_216334 (CHEMBL818748) Inhibition of specific binding of [3H]BK to bradykinin B2 receptors of guinea pig ileum (GPI)
- ChEMBL_216335 (CHEMBL818749) Inhibition of specific binding of [3H]BK to bradykinin B2 receptors of guinea pig ileum (GPI)
- ChEMBL_306532 (CHEMBL827821) Antagonist activity against human Bradykinin receptor B1 was determined in a fluorescence imaging plate reader assay
- ChEMBL_40267 (CHEMBL656503) Concentration required to inhibit specific binding of [3H]-BK(0.06 nM) to the bradykinin receptor B2
- ChEMBL_40284 (CHEMBL653416) Antagonism of the [Ca2+] efflux actions of the human Bradykinin receptor B2 (SK-N-SH neuroblastoma)
- ChEMBL_40430 (CHEMBL876526) Displacement of [3H]BK (1 nM) from human Bradykinin receptor B2 expressed in Cos-7 cells
- ChEMBL_423668 (CHEMBL913433) Displacement of [3H]des-Arg10 Leu9 kallidin from human bradykinin B1 receptor expressed in CHO cells
- ChEMBL_429973 (CHEMBL917703) Displacement of [3H]des-arg10, leu9-kallidin from human bradykinin B1 receptor expressed in CHO cells
- ChEMBL_446484 (CHEMBL895596) Antagonist activity at human bradykinin B1 receptor in IL1-beta stimulated IMR90 cells by FLIPR assay
- ChEMBL_512956 (CHEMBL977292) Displacement of [3H]DAK from human bradykinin B1 receptor expressed in clone CHO-D-/aequorin cells
- ChEMBL_662792 (CHEMBL1252531) Displacement of [3H]Lys0-des-Arg9-BK at human bradykinin B1 receptor expressed in HEK293 cells
- ChEMBL_40291 (CHEMBL653423) Inhibition of [3H]BK (1.0 nM) binding to the human bradykinin receptor B2, expressed in CHO cells
- ChEMBL_40419 (CHEMBL652634) Compound was assayed for binding against the human Bradykinin receptor B2 expressed in CHO cells; 0.2-16
- ChEMBL_40421 (CHEMBL652636) Affinity to human Bradykinin receptor B2 in CHO cell membranes determined by displacement of [3H]-NPC 17731
- ChEMBL_425235 (CHEMBL855800) Antagonistic activity at African green monkey bradykinin B1 receptor assessed as effect on DAK-mediated calcium mobilization
- ChEMBL_572639 (CHEMBL1026063) Antagonist activity at B2 receptor in human HF15 cells assessed as inhibition of bradykinin-induced calcium mobilization
- ChEMBL_644657 (CHEMBL1211636) Antagonist activity at human bradykinin B1 receptor assessed as inhibition of Lys-desArg9-BK-induced calcium flux
- ChEMBL_662795 (CHEMBL1252534) Antagonist activity at human bradykinin B1 receptor in human MR5 cells assessed as [3H]inositol phosphate accumulation
- ChEMBL_796434 (CHEMBL1937749) Antagonist activity at human B1 bradykinin receptor expressed in CHO cells by aqueorin-based calcium flux assay
- ChEMBL_965477 (CHEMBL2395281) Displacement of [3H](Des-Arg10)-Kallidin from bradykinin B1 receptor in human IMR90 cells after 60 mins
- ChEMBL_40274 (CHEMBL656509) Inhibition of the specific binding of [3H]BK to Bradykinin receptor B2 in guinea pig ileum membrane preparations
- ChEMBL_40294 (CHEMBL884128) Inhibition of the specific binding of [3H]BK to human recombinant Bradykinin receptor B2 expressed in CHO cells.
- ChEMBL_40438 (CHEMBL652377) Inhibition of increase in [Ca2+] efflux from NG108-15 cells caused by activation of rat Bradykinin receptor B2
- ChEMBL_512957 (CHEMBL977293) Antagonist activity at human bradykinin B1 receptor expressed in clone CHO-D-/aequorin cells by aquerin based assay
- ChEMBL_512960 (CHEMBL977296) Antagonist activity at rabbit bradykinin B1 receptor expressed in clone CHO-D-/aequorin cells by aquerin based assay
- ChEMBL_302253 (CHEMBL830269) Equilibrium dissociation constant of the [35S]- radiolabeled compound against human Bradykinin receptor B1 expressed in CHO membranes was determined
- ChEMBL_425210 (CHEMBL855156) Antagonistic activity at human bradykinin B1 receptor expressed in CHO cells assessed as effect on DAK-mediated calcium mobilization
- ChEMBL_434361 (CHEMBL919420) Antagonist activity at human bradykinin B1 receptor expressed in CHOD cells assessed as effect on DAK-induced calcium flux
- ChEMBL_510231 (CHEMBL1005609) Displacement of [3H]DAK from human bradykinin B1 receptor expressed in CHO-D-/aequorin cells by rapid filtration technique
- ChEMBL_535280 (CHEMBL982605) Antagonist activity at Cynomolgus monkey bradykinin B1 receptor expressed in CHO cells assessed as calcium transient by FLIPR assay
- ChEMBL_756380 (CHEMBL1805406) Antagonist activity at human bradykinin B1 receptor expressed in human HEK293 cells assessed as calcium flux by FLIPR assay
- ChEBML_40107 Binding affinity towards human bradykinin B2 receptor (membranes from Cos-7 cells expressing human B2 receptor) using [3H]-BK as radioligand
- ChEMBL_303697 (CHEMBL828184) Binding affinity to human Bradykinin receptor B1 over-expressed in transgenic rats was determined by ex vivo receptor occupancy assay
- ChEMBL_303698 (CHEMBL828185) Binding affinity to human Bradykinin receptor B2 over-expressed in transgenic rats was determined by ex vivo receptor occupancy assay
- ChEMBL_40443 (CHEMBL652382) Inhibition of binding of [3H]BK to rat bradykinin B2 receptor expressed in NG108-15 neuroblastoma-glioma hybrid cell membranes
- ChEMBL_425213 (CHEMBL855159) Antagonistic activity at rabbit bradykinin B1 receptor expressed in CHO-D cells assessed as effect on DAK-mediated calcium mobilization
- ChEMBL_492574 (CHEMBL952241) Displacement of [3H]des-arg10leu9kallidin from human bradykinin B1 receptor expressed in CHO cells by Wallac beta-plate scintillation counting
- ChEMBL_1560590 (CHEMBL3777322) Displacement of [3H]BK from cloned human B2 bradykinin receptor expressed in CHO cells after 2 hrs by liquid scintillation counter
- ChEMBL_40269 (CHEMBL856079) Concentration required to inhibit specific binding of [3H]-BK(0.06 nM) to the bradykinin receptor B2 in guinea pig ileum membrane
- ChEMBL_40292 (CHEMBL653424) In vitro inhibitory activity towards human bradykinin receptor B2 expressed in CHO cells using [3H]BK (1.0 nM) as a radioligand
- ChEMBL_40293 (CHEMBL653425) Inhibition of specific binding of [3H]BK at 1 nM to human bradykinin receptor B2 expressed in CHO cells by 50%.
- ChEMBL_40444 (CHEMBL652383) Inhibition of specific binding of [3H]-BK (1 nM) to rat Bradykinin receptor B2 by 50% in NG108-15 cell membranes
- ChEMBL_852821 (CHEMBL2155420) Antagonist activity at human bradykinin B1 receptor expressed in human CHO cells assessed as inhibition of calcium flux by FLIPR assay
- ChEBML_40436 In vitro binding affinity against Bradykinin receptor B2 in rat NG 108-15 neuroblastoma-glioma hybrid cell membranes using [3H]BK binding assay
- ChEMBL_40262 (CHEMBL653278) In vitro for inhibition of specific binding of [3H]BK (0.06 nM) to bradykinin receptor B2 in guinea pig ileum membrane preparations.
- ChEMBL_40272 (CHEMBL656507) In vitro inhibitory activity towards bradykinin receptor B2 using [3H]BK (0.06 nM) as a radioligand in guinea pig ileum membrane preparation
- ChEMBL_40273 (CHEMBL656508) Inhibition of specific binding of [3H]BK at 0.06 nM to bradykinin receptor B2 in guinea pig ileum membrane preparations by 50%.
- ChEMBL_612393 (CHEMBL1066279) Antagonist activity at bradykinin B1 receptor in human IMR90 cells pretreated with IL1-beta assessed as inhibition of DAKD-induced calcium mobilization
- ChEMBL_797691 (CHEMBL1943911) Displacement of [3H]-DAK from human bradykinin B1 receptor expressed in CHO-D-/aequorin cells membrane after 90 mins by scintillation counting
- ChEMBL_1550090 (CHEMBL3756036) Inhibition of Pseudomonas aeruginosa pseudolysin pretreated with compound for 1 hr followed by the addition of 1.73 uM bradykinin like substrate by spectrofluorometry
- ChEMBL_40263 (CHEMBL653279) Concentration required to inhibit specific binding of [ 3H]BK (0.06 nM) to Bradykinin receptor B2 in guinea pig ileum membrane preparations by 50%
- ChEMBL_40265 (CHEMBL656501) Concentration required to inhibit specific binding of [ 3H]BK (0.06 nM) to Bradykinin receptor B2 in guinea pig ileum membrane preparations by 50%.
- ChEMBL_40436 (CHEMBL883337) In vitro binding affinity against Bradykinin receptor B2 in rat NG 108-15 neuroblastoma-glioma hybrid cell membranes using [3H]BK binding assay
- ChEMBL_423671 (CHEMBL912896) Activity at human bradykinin B1 receptor assessed as inhibition of Des-arg kallidin-induced increase of cytosolic calcium in CHO cells by FLIPR
- ChEMBL_748609 (CHEMBL1780462) Antagonist activity at human bradykinin B1 receptor expressed in CHO cells assessed as inhibition of agonist-induced calcium efflux by aquerin based assay
- ChEMBL_1550092 (CHEMBL3756038) Inhibition of Bacillus thermoproteolyticus thermolysin pretreated with compound for 1 hr followed by the addition of 3.33 uM bradykinin like substrate by spectrofluorometry assay
- ChEMBL_40264 (CHEMBL653280) Concentration required to inhibit specific binding of [3H]BK at 0.06 nM to Bradykinin receptor B2 in guinea pig ileum membrane preparations by 50%.
- ChEMBL_40286 (CHEMBL653418) Inhibition specific binding of [3H]BK (1.0 nM) to human Bradykinin receptor B2 which was expressed in CHO (Chinese hamster ovary) cells by 50%.
- ChEMBL_303777 (CHEMBL830134) Binding affinity of the [35S]- radiolabeled compound to human Bradykinin receptor B1 over-expressed in transgenic rats was determined by ex vivo receptor occupancy assay
- ChEMBL_303778 (CHEMBL830135) Binding affinity of the [35S]- radiolabeled compound to human Bradykinin receptor B2 over-expressed in transgenic rats was determined by ex vivo receptor occupancy assay
- ChEMBL_40289 (CHEMBL653421) Concentration required to inhibit specific binding of [3H]BK (1.2 nM) to A-431 cells (human epidermoid carcinoma) which express Bradykinin receptor B2 by 50%.
- ChEMBL_40288 (CHEMBL653420) Concentration required to inhibit specific binding of [3H]BK at 1.2 nM to A-431 cells (human epidermoid carcinoma) which express Bradykinin receptor B2 by 50%.
- ChEMBL_429974 (CHEMBL917704) Antagonist activity at bradykinin B1 receptor expressed in CHO cells assessed as inhibition of des-arg10-kallidin-induced increase in cytosolic calcium level by FLIPR assay
- ChEMBL_797692 (CHEMBL1943912) Antagonist activity at human bradykinin B1 receptor expressed in CHO-D-/aequorin cells assessed as inhibition of DAK-induced intracellular calcium level after 1.5 to 2 hrs by luminometry analysis
- ChEMBL_1651749 (CHEMBL4001004) Antagonist activity against bradykinin B1 receptor in human HeLa cells assessed as inhibition of Des-Arg9-BK-induced increase in intracellular Ca2+ level by Fluro-4 direct calcium dye based fluorescence assay
- ChEMBL_1687679 (CHEMBL4038158) Inhibition of human plasma kallikrein spiked in pig vitreous using HMWK as substrate assessed as suppression of bradykinin release preincubated for 15 mins followed by substrate addition measured after 15 mins by ELISA
- ChEMBL_1687677 (CHEMBL4038156) Inhibition of plasma kallikrein in human plasma using HMWK as substrate assessed as suppression of kaolin-activated protein induced bradykinin release preincubated for 15 mins followed by substrate addition measured after 15 min by ELISA
- ChEMBL_863255 (CHEMBL2176198) Inhibition of human recombinant Myc-His10-tagged cathepsin A expressed in baculovirus infected Sf9 cells using BodipyFL labeled bradykinin as substrate incubated for 15 mins prior to substrate addition measured after 15 mins by fluorimetric analysis
- Binding Assay For binding, Bradykinin-1 receptor antagonist compounds were added in various concentrations in 50 mM Tris pH 7.4, 5 mM MgCl2 together with 6 nM Kallidin (Des Arg10, Leu9), [3,4-Prolyl-3,4-3H(N)] (PerkinElmer, 1.85-4.44 TBq/mmol) to 40 μg membrane protein containing approximately 1 fmol Bradykinin-1 receptor and incubated for 15 min at 27° C. To determine non-specific binding 10 μM Lys-(Des-Arg9)-Bradykinin (Bachem) was added. Membranes were harvested through GF/B (glass fiber filter; PerkinElmer) plates, equilibrated with 0.5% polyethylenimine, air dried at 50° C. for 2 hr. Radioactivity was determined by counting in a topcounter (NXT Packard). Specific binding was defined as total binding minus nonspecific binding and typically represents about 90-95% of the total binding. Antagonist activity is expressed as Ki: inhibitor concentration required for 50% inhibition of specific binding corrected for the concentration of the radioligand.
- Inhibition Assay The activated cathepsin A was diluted in assay buffer (25 mM MES, pH 5.5, containing 5 mM DTT) and mixed with the test compound (dissolved in assay buffer containing (v/v) 3% DMSO) or, in the control experiments, with the vehicle in a multiple assay plate. After incubation for 15 min at room temperature, as substrate then bradykinin carrying an N-terminal Bodipy FL (4,4-difluoro-5,7-dimethyl-4-bora-3a,4a-diaza-s-indacene-3-propionyl) label (JPT Peptide Technologies GmbH; dissolved in assay buffer) was added to the mixture. The final concentration of cathepsin A was 833 ng/ml and the final concentration of labeled bradykinin 2 μM. After incubation for 15 min at room temperature the reaction was stopped by the addition of stop buffer (130 mM 2-(4-(2-hydroxy-ethyl)-piperazin-1-yl)-ethanesulfonic acid, pH 7.4, containing (v/v) 0.013% Triton X-100, 0.13% Coating Reagent 3 (Caliper Life Sciences), 6.5% DMSO and 20 μM ebelactone B (Sigma, #E0886)).
- Inhibition Assay The activated cathepsin A was diluted in assay buffer (25 mM MES, pH 5.5, containing 5 mM DTT) and mixed with the test compound (dissolved in assay buffer containing (v/v) 3% DMSO) or, in the control experiments, with the vehicle in a multiple assay plate. After incubation for 15 min at room temperature, as substrate then bradykinin carrying an N-terminal Bodipy FL (4,4-difluoro-5,7-dimethyl-4-bora-3a,4a-diaza-s-indacene-3-propionyl) label (JPT Peptide Technologies GmbH; dissolved in assay buffer) was added to the mixture. The final concentration of cathepsin A was 833 ng/ml and the final concentration of labeled bradykinin 2 μM. After incubation for 15 min at room temperature the reaction was stopped by the addition of stop buffer (130 mM 2-(4-(2-hydroxy-ethyl)-piperazin-1-yl)-ethanesulfonic acid, pH 7.4, containing (v/v) 0.013%° Triton X-100, 0.13% Coating Reagent 3 (Caliper Life Sciences), 6.5% DMSO and 20 μM ebelactone B (Sigma, #E0886)).
- Calcium Flux Assays (hB1 IC50 IMR90) Notably, Compound Examples are tested in the FLIPR assays in the presence (hB1 free IC50) of 0.1% BSA in assay buffer, in order to assess the potency shifts due to serum protein binding of Compound Examples. The effect of BSA on the potency of endothelin receptor antagonists have been described in the prior art (Wu-Wong, J. R. et al. (1997), JPET 281: 791-798). The teaching can be applied in analogy to testing the potency of Bradykinin B1 receptor antagonist in the FLIPR assays. For the calcium flux assay, 80% confluent cells are detached from the culture vessels with Versene (Gibco), and seeded into 384-well plates (Cell binding Surface; Corning, N.Y.; #3683) at a density of 15,000 cells per well. Cells are seeded in a volume of 50 μL in medium without antibiotics and incubated overnight in a humidified atmosphere with 5% CO2 at 37° C. The following day, the medium is replaced with 20 μL of 5 μM Fluo-4AM dye (Molecular Probes) in assay buffer (2.5 mM probenicid, 1 mg/mL pluronic acid, 135 mM NaCl, 5 mM KCl, 1.8 mM CaCl, 1 mM MgCl2, 10 mM HEPES, 5.6 mM glucose, and 0.05% gelatine, pH 7.4), which contains or lacks 0.1% BSA for determination of compound potency units as hB1 IC50 or hB1 free IC50, respectively. The calcium indicator loaded cells are incubated at 37° C. for 2 hrs. Extracellular dye is then removed and each well is filled with 45 μL of assay buffer. Cell plates are kept in dark until used. Compound examples are assayed at 8 concentrations in triplicate. Serial 10-fold dilutions in 100% DMSO are made at a 100-times higher concentration than the final concentration, and then diluted 1:10 in assay buffer. 5 μL of each diluted compound is added to the well of cell plates (yielding final concentration with 1% DMSO), and incubated for 30 min at 28° C. before the addition of Bradykinin B1 receptor agonist on the FLIPR instrument. Agonist plates contain the agonist Lys-(Des-Arg)-Bradykinin (Bachem, Brackley) at 3.5×EC90 in assay buffer with 1% DMSO. The addition of agonist 20 μl per well to the assay plate is carried out on the FLIPR instrument while continuously monitoring Ca2+-dependent fluorescence at 538 nm. A peptide antagonist Lys-(Des-Arg-Leu)-Bradykinin (Bachem, Brackley) at 20 □M is used to determine the full inhibition as control. Peak fluorescence is used to determine the response to agonist obtained at each concentration of Compound Examples by the following equation: % Response=100*(RFU(compound)−RFU(control))/(RFU(DMSO)−RFU(control)) RFU means relative fluorescence units. Control means full inhibition by the peptide antagonist Lys-(Des-Arg-Leu)-Bradykinin at 20 □M.The response values are plotted against the logarithm of the compound concentrations. The Compound Examples are tested in triplicates per plate and mean values are plotted in Excel XLfit to determine IC50 values, percentage of maximal inhibition and the Hill slopes.
- Calcium Flux Assays (hB1 IC50 free) Notably, Compound Examples are tested in the FLIPR assays in the absence (hB1 free IC50) of 0.1% BSA in assay buffer, in order to assess the potency shifts due to serum protein binding of Compound Examples. The effect of BSA on the potency of endothelin receptor antagonists have been described in the prior art (Wu-Wong, J. R. et al. (1997), JPET 281: 791-798). The teaching can be applied in analogy to testing the potency of Bradykinin B1 receptor antagonist in the FLIPR assays. For the calcium flux assay, 80% confluent cells are detached from the culture vessels with Versene (Gibco), and seeded into 384-well plates (Cell binding Surface; Corning, N.Y.; #3683) at a density of 15,000 cells per well. Cells are seeded in a volume of 50 μL in medium without antibiotics and incubated overnight in a humidified atmosphere with 5% CO2 at 37° C. The following day, the medium is replaced with 20 μL of 5 μM Fluo-4AM dye (Molecular Probes) in assay buffer (2.5 mM probenicid, 1 mg/mL pluronic acid, 135 mM NaCl, 5 mM KCl, 1.8 mM CaCl, 1 mM MgCl2, 10 mM HEPES, 5.6 mM glucose, and 0.05% gelatine, pH 7.4), which contains or lacks 0.1% BSA for determination of compound potency units as hB1 IC50 or hB1 free IC50, respectively. The calcium indicator loaded cells are incubated at 37° C. for 2 hrs. Extracellular dye is then removed and each well is filled with 45 μL of assay buffer. Cell plates are kept in dark until used. Compound examples are assayed at 8 concentrations in triplicate. Serial 10-fold dilutions in 100% DMSO are made at a 100-times higher concentration than the final concentration, and then diluted 1:10 in assay buffer. 5 μL of each diluted compound is added to the well of cell plates (yielding final concentration with 1% DMSO), and incubated for 30 min at 28° C. before the addition of Bradykinin B1 receptor agonist on the FLIPR instrument. Agonist plates contain the agonist Lys-(Des-Arg)-Bradykinin (Bachem, Brackley) at 3.5×EC90 in assay buffer with 1% DMSO. The addition of agonist 20 μl per well to the assay plate is carried out on the FLIPR instrument while continuously monitoring Ca2+-dependent fluorescence at 538 nm. A peptide antagonist Lys-(Des-Arg-Leu)-Bradykinin (Bachem, Brackley) at 20 □M is used to determine the full inhibition as control. Peak fluorescence is used to determine the response to agonist obtained at each concentration of Compound Examples by the following equation: % Response=100*(RFU(compound)−RFU(control))/(RFU(DMSO)−RFU(control)) RFU means relative fluorescence units. Control means full inhibition by the peptide antagonist Lys-(Des-Arg-Leu)-Bradykinin at 20 □M.The response values are plotted against the logarithm of the compound concentrations. The Compound Examples are tested in triplicates per plate and mean values are plotted in Excel XLfit to determine IC50 values, percentage of maximal inhibition and the Hill slopes.