Ligand source activities (1 row/activity)
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 122227 | 1378 | None | 24 | Rat | Functional | pEC50 | = | 7.1 | 7.1 | -97 | 3 | Compound was evaluated for agonist activity against B1 receptor in rat ileum longitudinal smooth muscleCompound was evaluated for agonist activity against B1 receptor in rat ileum longitudinal smooth muscle |
ChEMBL | None | None | None | None | 10.1016/S0960-894X(97)10042-7 | ||||
| 3825 | 1378 | None | 24 | Rat | Functional | pEC50 | = | 7.1 | 7.1 | -97 | 3 | Compound was evaluated for agonist activity against B1 receptor in rat ileum longitudinal smooth muscleCompound was evaluated for agonist activity against B1 receptor in rat ileum longitudinal smooth muscle |
ChEMBL | None | None | None | None | 10.1016/S0960-894X(97)10042-7 | ||||
| 644 | 1378 | None | 24 | Rat | Functional | pEC50 | = | 7.1 | 7.1 | -97 | 3 | Compound was evaluated for agonist activity against B1 receptor in rat ileum longitudinal smooth muscleCompound was evaluated for agonist activity against B1 receptor in rat ileum longitudinal smooth muscle |
ChEMBL | None | None | None | None | 10.1016/S0960-894X(97)10042-7 | ||||
| CHEMBL264100 | 1378 | None | 24 | Rat | Functional | pEC50 | = | 7.1 | 7.1 | -97 | 3 | Compound was evaluated for agonist activity against B1 receptor in rat ileum longitudinal smooth muscleCompound was evaluated for agonist activity against B1 receptor in rat ileum longitudinal smooth muscle |
ChEMBL | None | None | None | None | 10.1016/S0960-894X(97)10042-7 | ||||
| 44323260 | 107071 | None | 0 | Rat | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | Compound was evaluated for agonist activity against B1 receptor in rat ileum longitudinal smooth muscleCompound was evaluated for agonist activity against B1 receptor in rat ileum longitudinal smooth muscle |
ChEMBL | 845 | 32 | 10 | 10 | 0.7 | NCCCC[C@H](N)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCCCCCCCCCCC(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O | 10.1016/S0960-894X(97)10042-7 | ||
| CHEMBL315388 | 107071 | None | 0 | Rat | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | Compound was evaluated for agonist activity against B1 receptor in rat ileum longitudinal smooth muscleCompound was evaluated for agonist activity against B1 receptor in rat ileum longitudinal smooth muscle |
ChEMBL | 845 | 32 | 10 | 10 | 0.7 | NCCCC[C@H](N)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCCCCCCCCCCC(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O | 10.1016/S0960-894X(97)10042-7 | ||
| 11757682 | 122106 | None | 0 | Human | Functional | pIC50 | = | 10.4 | 10.4 | - | 1 | Antagonist activity against human Bradykinin receptor B1 was determined in a fluorescence imaging plate reader assayAntagonist activity against human Bradykinin receptor B1 was determined in a fluorescence imaging plate reader assay |
ChEMBL | 567 | 8 | 3 | 6 | 3.5 | O=C(C[C@@H]1C(=O)Nc2ccccc2N1S(=O)(=O)c1ccc2ccccc2c1)NCCc1ccc(C2=NCCN2)cc1 | 10.1016/j.bmcl.2004.09.074 | ||
| CHEMBL359553 | 122106 | None | 0 | Human | Functional | pIC50 | = | 10.4 | 10.4 | - | 1 | Antagonist activity against human Bradykinin receptor B1 was determined in a fluorescence imaging plate reader assayAntagonist activity against human Bradykinin receptor B1 was determined in a fluorescence imaging plate reader assay |
ChEMBL | 567 | 8 | 3 | 6 | 3.5 | O=C(C[C@@H]1C(=O)Nc2ccccc2N1S(=O)(=O)c1ccc2ccccc2c1)NCCc1ccc(C2=NCCN2)cc1 | 10.1016/j.bmcl.2004.09.074 | ||
| 11214480 | 149267 | None | 0 | Human | Functional | pIC50 | = | 10.1 | 10.1 | - | 1 | Antagonist activity at human bradykinin B1 receptor in IL1-beta stimulated IMR90 cells by FLIPR assayAntagonist activity at human bradykinin B1 receptor in IL1-beta stimulated IMR90 cells by FLIPR assay |
ChEMBL | 514 | 7 | 4 | 5 | 4.3 | O=C(Nc1[nH]nc(C(=O)Nc2ccc(CCC3=NCCN3)cc2)c1Br)c1ccccc1Cl | 10.1021/jm051292n | ||
| CHEMBL394370 | 149267 | None | 0 | Human | Functional | pIC50 | = | 10.1 | 10.1 | - | 1 | Antagonist activity at human bradykinin B1 receptor in IL1-beta stimulated IMR90 cells by FLIPR assayAntagonist activity at human bradykinin B1 receptor in IL1-beta stimulated IMR90 cells by FLIPR assay |
ChEMBL | 514 | 7 | 4 | 5 | 4.3 | O=C(Nc1[nH]nc(C(=O)Nc2ccc(CCC3=NCCN3)cc2)c1Br)c1ccccc1Cl | 10.1021/jm051292n | ||
| 57397292 | 70081 | None | 0 | Human | Functional | pIC50 | = | 10.1 | 10.1 | - | 1 | 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 analysisAntagonist 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 | 522 | 7 | 2 | 5 | 3.1 | Cc1ccc(S(=O)(=O)N2C=CNC(=O)[C@H]2CC(=O)N[C@@H]2CCCc3cc(CN4CCCC4)ccc32)cc1 | 10.1016/j.bmcl.2011.11.112 | ||
| CHEMBL1939758 | 70081 | None | 0 | Human | Functional | pIC50 | = | 10.1 | 10.1 | - | 1 | 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 analysisAntagonist 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 | 522 | 7 | 2 | 5 | 3.1 | Cc1ccc(S(=O)(=O)N2C=CNC(=O)[C@H]2CC(=O)N[C@@H]2CCCc3cc(CN4CCCC4)ccc32)cc1 | 10.1016/j.bmcl.2011.11.112 | ||
| 54772237 | 65804 | None | 0 | Human | Functional | pIC50 | = | 10.1 | 10.1 | 6 | 2 | Antagonist activity at human B1 receptor expressed in CHO cells by aequorin-based calcium flux assayAntagonist activity at human B1 receptor expressed in CHO cells by aequorin-based calcium flux assay |
ChEMBL | 525 | 5 | 1 | 6 | 5.0 | Cc1nn(-c2ccc(C(=O)N[C@@H]3CCCc4cc(CN5CCCCC5)ccc43)cn2)c(=O)c2c(F)cccc12 | 10.1021/jm200808v | ||
| CHEMBL1834752 | 65804 | None | 0 | Human | Functional | pIC50 | = | 10.1 | 10.1 | 6 | 2 | Antagonist activity at human B1 receptor expressed in CHO cells by aequorin-based calcium flux assayAntagonist activity at human B1 receptor expressed in CHO cells by aequorin-based calcium flux assay |
ChEMBL | 525 | 5 | 1 | 6 | 5.0 | Cc1nn(-c2ccc(C(=O)N[C@@H]3CCCc4cc(CN5CCCCC5)ccc43)cn2)c(=O)c2c(F)cccc12 | 10.1021/jm200808v | ||
| 60142570 | 125982 | None | 0 | Human | Functional | pIC50 | = | 10 | 10.0 | - | 1 | Calcium Mobilization Assay: Calcium mobilization assay using Bradykinin-1 receptor.Calcium Mobilization Assay: Calcium mobilization assay using Bradykinin-1 receptor. |
ChEMBL | 532 | 6 | 2 | 7 | 4.4 | Cc1nc(-c2c(F)cc(Cl)cc2-c2ccc3c(c2)CC[C@@H]3NC(=O)C2(NC(=O)c3cncnc3)CC2)no1 | nan | ||
| CHEMBL3648475 | 125982 | None | 0 | Human | Functional | pIC50 | = | 10 | 10.0 | - | 1 | Calcium Mobilization Assay: Calcium mobilization assay using Bradykinin-1 receptor.Calcium Mobilization Assay: Calcium mobilization assay using Bradykinin-1 receptor. |
ChEMBL | 532 | 6 | 2 | 7 | 4.4 | Cc1nc(-c2c(F)cc(Cl)cc2-c2ccc3c(c2)CC[C@@H]3NC(=O)C2(NC(=O)c3cncnc3)CC2)no1 | nan | ||
| 60142706 | 125987 | None | 0 | Human | Functional | pIC50 | = | 10 | 10.0 | - | 1 | Calcium Mobilization Assay: Calcium mobilization assay using Bradykinin-1 receptor.Calcium Mobilization Assay: Calcium mobilization assay using Bradykinin-1 receptor. |
ChEMBL | 551 | 7 | 2 | 8 | 4.6 | COc1cc(C(=O)NC2(C(=O)N[C@H]3CCc4cc(-c5cc(Cl)cc(F)c5-c5noc(C)n5)ccc43)CC2)on1 | nan | ||
| CHEMBL3648480 | 125987 | None | 0 | Human | Functional | pIC50 | = | 10 | 10.0 | - | 1 | Calcium Mobilization Assay: Calcium mobilization assay using Bradykinin-1 receptor.Calcium Mobilization Assay: Calcium mobilization assay using Bradykinin-1 receptor. |
ChEMBL | 551 | 7 | 2 | 8 | 4.6 | COc1cc(C(=O)NC2(C(=O)N[C@H]3CCc4cc(-c5cc(Cl)cc(F)c5-c5noc(C)n5)ccc43)CC2)on1 | nan | ||
| 11570120 | 70078 | None | 0 | Human | Functional | pIC50 | = | 9.9 | 9.9 | - | 1 | 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 analysisAntagonist 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 | 536 | 7 | 2 | 5 | 3.5 | Cc1ccc(S(=O)(=O)N2C=CNC(=O)[C@H]2CC(=O)N[C@@H]2CCCc3cc(CN4CCCCC4)ccc32)cc1 | 10.1016/j.bmcl.2011.11.112 | ||
| CHEMBL1939755 | 70078 | None | 0 | Human | Functional | pIC50 | = | 9.9 | 9.9 | - | 1 | 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 analysisAntagonist 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 | 536 | 7 | 2 | 5 | 3.5 | Cc1ccc(S(=O)(=O)N2C=CNC(=O)[C@H]2CC(=O)N[C@@H]2CCCc3cc(CN4CCCCC4)ccc32)cc1 | 10.1016/j.bmcl.2011.11.112 | ||
| 24970287 | 188530 | None | 0 | Human | Functional | pIC50 | = | 9.9 | 9.9 | - | 1 | Antagonist activity at human bradykinin B1 receptor expressed in CHO-D-/aequorin cellsAntagonist activity at human bradykinin B1 receptor expressed in CHO-D-/aequorin cells |
ChEMBL | 574 | 7 | 2 | 6 | 4.2 | O=C(C[C@@H]1C(=O)Nc2ccccc2N1S(=O)(=O)c1ccccc1)N[C@@H]1CCOc2cc(CN3CCCCC3)ccc21 | 10.1016/j.bmcl.2008.07.055 | ||
| CHEMBL502140 | 188530 | None | 0 | Human | Functional | pIC50 | = | 9.9 | 9.9 | - | 1 | Antagonist activity at human bradykinin B1 receptor expressed in CHO-D-/aequorin cellsAntagonist activity at human bradykinin B1 receptor expressed in CHO-D-/aequorin cells |
ChEMBL | 574 | 7 | 2 | 6 | 4.2 | O=C(C[C@@H]1C(=O)Nc2ccccc2N1S(=O)(=O)c1ccccc1)N[C@@H]1CCOc2cc(CN3CCCCC3)ccc21 | 10.1016/j.bmcl.2008.07.055 | ||
| 46230121 | 204601 | None | 0 | Human | Functional | pIC50 | = | 9.9 | 9.9 | - | 1 | Antagonist activity at bradykinin B1 receptor in human IMR90 cells assessed as inhibition of des-Arg-bradykinin-mediated calcium mobilizationAntagonist activity at bradykinin B1 receptor in human IMR90 cells assessed as inhibition of des-Arg-bradykinin-mediated calcium mobilization |
ChEMBL | 546 | 7 | 2 | 9 | 3.3 | CCN(NC(=O)c1cc(OC)no1)C(=O)NCc1ccc(-c2cc(Cl)cc(F)c2-c2nnn(C)n2)cc1F | 10.1016/j.bmcl.2009.11.119 | ||
| CHEMBL609157 | 204601 | None | 0 | Human | Functional | pIC50 | = | 9.9 | 9.9 | - | 1 | Antagonist activity at bradykinin B1 receptor in human IMR90 cells assessed as inhibition of des-Arg-bradykinin-mediated calcium mobilizationAntagonist activity at bradykinin B1 receptor in human IMR90 cells assessed as inhibition of des-Arg-bradykinin-mediated calcium mobilization |
ChEMBL | 546 | 7 | 2 | 9 | 3.3 | CCN(NC(=O)c1cc(OC)no1)C(=O)NCc1ccc(-c2cc(Cl)cc(F)c2-c2nnn(C)n2)cc1F | 10.1016/j.bmcl.2009.11.119 | ||
| 46230161 | 203877 | None | 0 | Human | Functional | pIC50 | = | 9.9 | 9.9 | - | 1 | Antagonist activity at bradykinin B1 receptor in human IMR90 cells assessed as inhibition of des-Arg-bradykinin-mediated calcium mobilizationAntagonist activity at bradykinin B1 receptor in human IMR90 cells assessed as inhibition of des-Arg-bradykinin-mediated calcium mobilization |
ChEMBL | 561 | 7 | 2 | 10 | 3.3 | CCN(NC(=O)c1cc(OC)no1)C(=O)N[C@H](C)c1ncc(-c2cc(Cl)cc(F)c2-c2nnn(C)n2)cc1F | 10.1016/j.bmcl.2009.11.119 | ||
| CHEMBL604735 | 203877 | None | 0 | Human | Functional | pIC50 | = | 9.9 | 9.9 | - | 1 | Antagonist activity at bradykinin B1 receptor in human IMR90 cells assessed as inhibition of des-Arg-bradykinin-mediated calcium mobilizationAntagonist activity at bradykinin B1 receptor in human IMR90 cells assessed as inhibition of des-Arg-bradykinin-mediated calcium mobilization |
ChEMBL | 561 | 7 | 2 | 10 | 3.3 | CCN(NC(=O)c1cc(OC)no1)C(=O)N[C@H](C)c1ncc(-c2cc(Cl)cc(F)c2-c2nnn(C)n2)cc1F | 10.1016/j.bmcl.2009.11.119 | ||
| 54582655 | 62216 | None | 0 | Human | Functional | pIC50 | = | 9.9 | 9.9 | - | 1 | Antagonist activity at human bradykinin B1 receptor expressed in CHO cells assessed as inhibition of agonist-induced calcium efflux by aquerin based assayAntagonist activity at human bradykinin B1 receptor expressed in CHO cells assessed as inhibition of agonist-induced calcium efflux by aquerin based assay |
ChEMBL | 552 | 7 | 2 | 5 | 3.3 | Cc1ccc(S(=O)(=O)N2CCNC(=O)[C@H]2CC(=O)N[C@@H]2CCCc3cc(CN4CCC(C)CC4)ccc32)cc1 | 10.1016/j.bmcl.2011.03.115 | ||
| CHEMBL1777969 | 62216 | None | 0 | Human | Functional | pIC50 | = | 9.9 | 9.9 | - | 1 | Antagonist activity at human bradykinin B1 receptor expressed in CHO cells assessed as inhibition of agonist-induced calcium efflux by aquerin based assayAntagonist activity at human bradykinin B1 receptor expressed in CHO cells assessed as inhibition of agonist-induced calcium efflux by aquerin based assay |
ChEMBL | 552 | 7 | 2 | 5 | 3.3 | Cc1ccc(S(=O)(=O)N2CCNC(=O)[C@H]2CC(=O)N[C@@H]2CCCc3cc(CN4CCC(C)CC4)ccc32)cc1 | 10.1016/j.bmcl.2011.03.115 | ||
| 44587189 | 172544 | None | 0 | Human | Functional | pIC50 | = | 9.9 | 9.9 | - | 1 | Antagonist activity at human bradykinin B1 receptor expressed in CHO-D-/aequorin cellsAntagonist activity at human bradykinin B1 receptor expressed in CHO-D-/aequorin cells |
ChEMBL | 588 | 7 | 2 | 6 | 4.5 | Cc1ccc(S(=O)(=O)N2c3ccccc3NC(=O)[C@H]2CC(=O)N[C@@H]2CCOc3cc(CN4CCCCC4)ccc32)cc1 | 10.1016/j.bmcl.2008.07.055 | ||
| CHEMBL447870 | 172544 | None | 0 | Human | Functional | pIC50 | = | 9.9 | 9.9 | - | 1 | Antagonist activity at human bradykinin B1 receptor expressed in CHO-D-/aequorin cellsAntagonist activity at human bradykinin B1 receptor expressed in CHO-D-/aequorin cells |
ChEMBL | 588 | 7 | 2 | 6 | 4.5 | Cc1ccc(S(=O)(=O)N2c3ccccc3NC(=O)[C@H]2CC(=O)N[C@@H]2CCOc3cc(CN4CCCCC4)ccc32)cc1 | 10.1016/j.bmcl.2008.07.055 | ||
| 56594769 | 65747 | None | 0 | Human | Functional | pIC50 | = | 9.7 | 9.7 | 6 | 2 | Antagonist activity at human B1 receptor expressed in CHO cells by aequorin-based calcium flux assayAntagonist activity at human B1 receptor expressed in CHO cells by aequorin-based calcium flux assay |
ChEMBL | 541 | 5 | 1 | 6 | 5.5 | Cc1nn(-c2ccc(C(=O)N[C@@H]3CCCc4cc(CN5CCCCC5)ccc43)cn2)c(=O)c2c(Cl)cccc12 | 10.1021/jm200808v | ||
| CHEMBL1834619 | 65747 | None | 0 | Human | Functional | pIC50 | = | 9.7 | 9.7 | 6 | 2 | Antagonist activity at human B1 receptor expressed in CHO cells by aequorin-based calcium flux assayAntagonist activity at human B1 receptor expressed in CHO cells by aequorin-based calcium flux assay |
ChEMBL | 541 | 5 | 1 | 6 | 5.5 | Cc1nn(-c2ccc(C(=O)N[C@@H]3CCCc4cc(CN5CCCCC5)ccc43)cn2)c(=O)c2c(Cl)cccc12 | 10.1021/jm200808v | ||
| 665 | 973 | None | 2 | Human | Functional | pIC50 | = | 9.7 | 9.7 | 1 | 4 | Antagonist activity at human bradykinin B1 receptor expressed in CHO-D-/aequorin cellsAntagonist activity at human bradykinin B1 receptor expressed in CHO-D-/aequorin cells |
ChEMBL | 585 | 8 | 3 | 6 | 3.6 | O=C(C[C@@H]1C(=O)Nc2c(N1S(=O)(=O)c1ccc(c(c1)Cl)Cl)cccc2)NCCc1ccc(cc1)C1=NCCN1 | 10.1016/j.bmcl.2008.07.055 | ||
| 9916412 | 973 | None | 2 | Human | Functional | pIC50 | = | 9.7 | 9.7 | 1 | 4 | Antagonist activity at human bradykinin B1 receptor expressed in CHO-D-/aequorin cellsAntagonist activity at human bradykinin B1 receptor expressed in CHO-D-/aequorin cells |
ChEMBL | 585 | 8 | 3 | 6 | 3.6 | O=C(C[C@@H]1C(=O)Nc2c(N1S(=O)(=O)c1ccc(c(c1)Cl)Cl)cccc2)NCCc1ccc(cc1)C1=NCCN1 | 10.1016/j.bmcl.2008.07.055 | ||
| CHEMBL189123 | 973 | None | 2 | Human | Functional | pIC50 | = | 9.7 | 9.7 | 1 | 4 | Antagonist activity at human bradykinin B1 receptor expressed in CHO-D-/aequorin cellsAntagonist activity at human bradykinin B1 receptor expressed in CHO-D-/aequorin cells |
ChEMBL | 585 | 8 | 3 | 6 | 3.6 | O=C(C[C@@H]1C(=O)Nc2c(N1S(=O)(=O)c1ccc(c(c1)Cl)Cl)cccc2)NCCc1ccc(cc1)C1=NCCN1 | 10.1016/j.bmcl.2008.07.055 | ||
| 665 | 973 | None | 2 | Human | Functional | pIC50 | = | 9.7 | 9.7 | 1 | 4 | Antagonist activity at human bradykinin B1 receptor in human MR5 cells assessed as [3H]inositol phosphate accumulationAntagonist activity at human bradykinin B1 receptor in human MR5 cells assessed as [3H]inositol phosphate accumulation |
ChEMBL | 585 | 8 | 3 | 6 | 3.6 | O=C(C[C@@H]1C(=O)Nc2c(N1S(=O)(=O)c1ccc(c(c1)Cl)Cl)cccc2)NCCc1ccc(cc1)C1=NCCN1 | 10.1021/jm1000776 | ||
| 9916412 | 973 | None | 2 | Human | Functional | pIC50 | = | 9.7 | 9.7 | 1 | 4 | Antagonist activity at human bradykinin B1 receptor in human MR5 cells assessed as [3H]inositol phosphate accumulationAntagonist activity at human bradykinin B1 receptor in human MR5 cells assessed as [3H]inositol phosphate accumulation |
ChEMBL | 585 | 8 | 3 | 6 | 3.6 | O=C(C[C@@H]1C(=O)Nc2c(N1S(=O)(=O)c1ccc(c(c1)Cl)Cl)cccc2)NCCc1ccc(cc1)C1=NCCN1 | 10.1021/jm1000776 | ||
| CHEMBL189123 | 973 | None | 2 | Human | Functional | pIC50 | = | 9.7 | 9.7 | 1 | 4 | Antagonist activity at human bradykinin B1 receptor in human MR5 cells assessed as [3H]inositol phosphate accumulationAntagonist activity at human bradykinin B1 receptor in human MR5 cells assessed as [3H]inositol phosphate accumulation |
ChEMBL | 585 | 8 | 3 | 6 | 3.6 | O=C(C[C@@H]1C(=O)Nc2c(N1S(=O)(=O)c1ccc(c(c1)Cl)Cl)cccc2)NCCc1ccc(cc1)C1=NCCN1 | 10.1021/jm1000776 | ||
| 46216675 | 203065 | None | 0 | Human | Functional | pIC50 | = | 9.7 | 9.7 | - | 1 | Antagonist activity at bradykinin B1 receptor in human IMR90 cells assessed as inhibition of des-Arg-bradykinin-mediated calcium mobilizationAntagonist activity at bradykinin B1 receptor in human IMR90 cells assessed as inhibition of des-Arg-bradykinin-mediated calcium mobilization |
ChEMBL | 513 | 5 | 2 | 7 | 4.3 | Cn1nnc(-c2c(F)cc(Cl)cc2-c2cnc(CNC(=O)N(O)C3CCC(F)(F)CC3)c(F)c2)n1 | 10.1016/j.bmcl.2009.11.121 | ||
| CHEMBL599285 | 203065 | None | 0 | Human | Functional | pIC50 | = | 9.7 | 9.7 | - | 1 | Antagonist activity at bradykinin B1 receptor in human IMR90 cells assessed as inhibition of des-Arg-bradykinin-mediated calcium mobilizationAntagonist activity at bradykinin B1 receptor in human IMR90 cells assessed as inhibition of des-Arg-bradykinin-mediated calcium mobilization |
ChEMBL | 513 | 5 | 2 | 7 | 4.3 | Cn1nnc(-c2c(F)cc(Cl)cc2-c2cnc(CNC(=O)N(O)C3CCC(F)(F)CC3)c(F)c2)n1 | 10.1016/j.bmcl.2009.11.121 | ||
| 46230160 | 203037 | None | 0 | Human | Functional | pIC50 | = | 9.7 | 9.7 | - | 1 | Antagonist activity at bradykinin B1 receptor in human IMR90 cells assessed as inhibition of des-Arg-bradykinin-mediated calcium mobilizationAntagonist activity at bradykinin B1 receptor in human IMR90 cells assessed as inhibition of des-Arg-bradykinin-mediated calcium mobilization |
ChEMBL | 547 | 7 | 2 | 10 | 2.7 | CCN(NC(=O)c1cc(OC)no1)C(=O)NCc1ncc(-c2cc(Cl)cc(F)c2-c2nnn(C)n2)cc1F | 10.1016/j.bmcl.2009.11.119 | ||
| CHEMBL599153 | 203037 | None | 0 | Human | Functional | pIC50 | = | 9.7 | 9.7 | - | 1 | Antagonist activity at bradykinin B1 receptor in human IMR90 cells assessed as inhibition of des-Arg-bradykinin-mediated calcium mobilizationAntagonist activity at bradykinin B1 receptor in human IMR90 cells assessed as inhibition of des-Arg-bradykinin-mediated calcium mobilization |
ChEMBL | 547 | 7 | 2 | 10 | 2.7 | CCN(NC(=O)c1cc(OC)no1)C(=O)NCc1ncc(-c2cc(Cl)cc(F)c2-c2nnn(C)n2)cc1F | 10.1016/j.bmcl.2009.11.119 | ||
| 11387387 | 62214 | None | 0 | Human | Functional | pIC50 | = | 9.7 | 9.7 | - | 1 | Antagonist activity at human bradykinin B1 receptor expressed in CHO cells assessed as inhibition of agonist-induced calcium efflux by aquerin based assayAntagonist activity at human bradykinin B1 receptor expressed in CHO cells assessed as inhibition of agonist-induced calcium efflux by aquerin based assay |
ChEMBL | 558 | 7 | 2 | 5 | 3.4 | O=C(C[C@@H]1C(=O)NCCN1S(=O)(=O)c1ccc(Cl)cc1)N[C@@H]1CCCc2cc(CN3CCCCC3)ccc21 | 10.1016/j.bmcl.2011.03.115 | ||
| CHEMBL1777967 | 62214 | None | 0 | Human | Functional | pIC50 | = | 9.7 | 9.7 | - | 1 | Antagonist activity at human bradykinin B1 receptor expressed in CHO cells assessed as inhibition of agonist-induced calcium efflux by aquerin based assayAntagonist activity at human bradykinin B1 receptor expressed in CHO cells assessed as inhibition of agonist-induced calcium efflux by aquerin based assay |
ChEMBL | 558 | 7 | 2 | 5 | 3.4 | O=C(C[C@@H]1C(=O)NCCN1S(=O)(=O)c1ccc(Cl)cc1)N[C@@H]1CCCc2cc(CN3CCCCC3)ccc21 | 10.1016/j.bmcl.2011.03.115 | ||
| 57523216 | 125983 | None | 0 | Human | Functional | pIC50 | = | 9.7 | 9.7 | - | 1 | Calcium Mobilization Assay: Calcium mobilization assay using Bradykinin-1 receptor.Calcium Mobilization Assay: Calcium mobilization assay using Bradykinin-1 receptor. |
ChEMBL | 562 | 7 | 2 | 8 | 4.4 | COc1ncc(C(=O)NC2(C(=O)N[C@H]3CCc4cc(-c5cc(Cl)cc(F)c5-c5noc(C)n5)ccc43)CC2)cn1 | nan | ||
| CHEMBL3648476 | 125983 | None | 0 | Human | Functional | pIC50 | = | 9.7 | 9.7 | - | 1 | Calcium Mobilization Assay: Calcium mobilization assay using Bradykinin-1 receptor.Calcium Mobilization Assay: Calcium mobilization assay using Bradykinin-1 receptor. |
ChEMBL | 562 | 7 | 2 | 8 | 4.4 | COc1ncc(C(=O)NC2(C(=O)N[C@H]3CCc4cc(-c5cc(Cl)cc(F)c5-c5noc(C)n5)ccc43)CC2)cn1 | nan | ||
| 60142962 | 125995 | None | 0 | Human | Functional | pIC50 | = | 9.7 | 9.7 | - | 1 | Calcium Mobilization Assay: Calcium mobilization assay using Bradykinin-1 receptor.Calcium Mobilization Assay: Calcium mobilization assay using Bradykinin-1 receptor. |
ChEMBL | 552 | 7 | 2 | 9 | 4.0 | COc1cc(C(=O)NC2(C(=O)NC3CCc4cc(-c5cc(Cl)cc(F)c5-c5noc(C)n5)cnc43)CC2)on1 | nan | ||
| CHEMBL3648488 | 125995 | None | 0 | Human | Functional | pIC50 | = | 9.7 | 9.7 | - | 1 | Calcium Mobilization Assay: Calcium mobilization assay using Bradykinin-1 receptor.Calcium Mobilization Assay: Calcium mobilization assay using Bradykinin-1 receptor. |
ChEMBL | 552 | 7 | 2 | 9 | 4.0 | COc1cc(C(=O)NC2(C(=O)NC3CCc4cc(-c5cc(Cl)cc(F)c5-c5noc(C)n5)cnc43)CC2)on1 | nan | ||
| 60142963 | 125996 | None | 0 | Human | Functional | pIC50 | = | 9.7 | 9.7 | - | 1 | Calcium Mobilization Assay: Calcium mobilization assay using Bradykinin-1 receptor.Calcium Mobilization Assay: Calcium mobilization assay using Bradykinin-1 receptor. |
ChEMBL | 533 | 6 | 2 | 8 | 3.8 | Cc1nc(-c2c(F)cc(Cl)cc2-c2cnc3c(c2)CCC3NC(=O)C2(NC(=O)c3ccnnc3)CC2)no1 | nan | ||
| CHEMBL3648489 | 125996 | None | 0 | Human | Functional | pIC50 | = | 9.7 | 9.7 | - | 1 | Calcium Mobilization Assay: Calcium mobilization assay using Bradykinin-1 receptor.Calcium Mobilization Assay: Calcium mobilization assay using Bradykinin-1 receptor. |
ChEMBL | 533 | 6 | 2 | 8 | 3.8 | Cc1nc(-c2c(F)cc(Cl)cc2-c2cnc3c(c2)CCC3NC(=O)C2(NC(=O)c3ccnnc3)CC2)no1 | nan | ||
Showing 1 to 50 of 1,247 entries
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 135398735 | 137055 | None | 20 | Human | Binding | pAC50 | = | 4.9 | 4.9 | - | 0 | Binding affinity towards human BDKRB1 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human BDKRB1 in an in vitro assay with cellular components measured by scintillation proximity assay |
ChEMBL | 822 | 4 | 6 | 15 | 4.3 | CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C | 10.1038/s41467-023-40064-9 | ||
| 136262914 | 137055 | None | 20 | Human | Binding | pAC50 | = | 4.9 | 4.9 | - | 0 | Binding affinity towards human BDKRB1 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human BDKRB1 in an in vitro assay with cellular components measured by scintillation proximity assay |
ChEMBL | 822 | 4 | 6 | 15 | 4.3 | CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C | 10.1038/s41467-023-40064-9 | ||
| CHEMBL374478 | 137055 | None | 20 | Human | Binding | pAC50 | = | 4.9 | 4.9 | - | 0 | Binding affinity towards human BDKRB1 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human BDKRB1 in an in vitro assay with cellular components measured by scintillation proximity assay |
ChEMBL | 822 | 4 | 6 | 15 | 4.3 | CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C | 10.1038/s41467-023-40064-9 | ||
| 644241 | 95239 | None | 68 | Human | Binding | pAC50 | = | 4.6 | 4.6 | - | 0 | Binding affinity towards human BDKRB1 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human BDKRB1 in an in vitro assay with cellular components measured by scintillation proximity assay |
ChEMBL | 529 | 6 | 2 | 7 | 6.4 | Cc1cn(-c2cc(NC(=O)c3ccc(C)c(Nc4nccc(-c5cccnc5)n4)c3)cc(C(F)(F)F)c2)cn1 | 10.1038/s41467-023-40064-9 | ||
| CHEMBL255863 | 95239 | None | 68 | Human | Binding | pAC50 | = | 4.6 | 4.6 | - | 0 | Binding affinity towards human BDKRB1 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human BDKRB1 in an in vitro assay with cellular components measured by scintillation proximity assay |
ChEMBL | 529 | 6 | 2 | 7 | 6.4 | Cc1cn(-c2cc(NC(=O)c3ccc(C)c(Nc4nccc(-c5cccnc5)n4)c3)cc(C(F)(F)F)c2)cn1 | 10.1038/s41467-023-40064-9 | ||
| 665 | 973 | None | 2 | Rabbit | Binding | pIC50 | = | 9.6 | 9.6 | - | 2 | Inhibition of rabbit bradykinin B1 receptorInhibition of rabbit bradykinin B1 receptor |
ChEMBL | 585 | 8 | 3 | 6 | 3.6 | O=C(C[C@@H]1C(=O)Nc2c(N1S(=O)(=O)c1ccc(c(c1)Cl)Cl)cccc2)NCCc1ccc(cc1)C1=NCCN1 | 10.1021/jm1000776 | ||
| 9916412 | 973 | None | 2 | Rabbit | Binding | pIC50 | = | 9.6 | 9.6 | - | 2 | Inhibition of rabbit bradykinin B1 receptorInhibition of rabbit bradykinin B1 receptor |
ChEMBL | 585 | 8 | 3 | 6 | 3.6 | O=C(C[C@@H]1C(=O)Nc2c(N1S(=O)(=O)c1ccc(c(c1)Cl)Cl)cccc2)NCCc1ccc(cc1)C1=NCCN1 | 10.1021/jm1000776 | ||
| CHEMBL189123 | 973 | None | 2 | Rabbit | Binding | pIC50 | = | 9.6 | 9.6 | - | 2 | Inhibition of rabbit bradykinin B1 receptorInhibition of rabbit bradykinin B1 receptor |
ChEMBL | 585 | 8 | 3 | 6 | 3.6 | O=C(C[C@@H]1C(=O)Nc2c(N1S(=O)(=O)c1ccc(c(c1)Cl)Cl)cccc2)NCCc1ccc(cc1)C1=NCCN1 | 10.1021/jm1000776 | ||
| 122227 | 1378 | None | 24 | Human | Binding | pIC50 | = | 9.1 | 9.1 | 6 | 3 | Displacement of [3H](Des-Arg10)-Kallidin from bradykinin B1 receptor in human IMR90 cells after 60 minsDisplacement of [3H](Des-Arg10)-Kallidin from bradykinin B1 receptor in human IMR90 cells after 60 mins |
ChEMBL | None | None | None | None | 10.1016/j.bmcl.2013.01.025 | ||||
| 3825 | 1378 | None | 24 | Human | Binding | pIC50 | = | 9.1 | 9.1 | 6 | 3 | Displacement of [3H](Des-Arg10)-Kallidin from bradykinin B1 receptor in human IMR90 cells after 60 minsDisplacement of [3H](Des-Arg10)-Kallidin from bradykinin B1 receptor in human IMR90 cells after 60 mins |
ChEMBL | None | None | None | None | 10.1016/j.bmcl.2013.01.025 | ||||
| 644 | 1378 | None | 24 | Human | Binding | pIC50 | = | 9.1 | 9.1 | 6 | 3 | Displacement of [3H](Des-Arg10)-Kallidin from bradykinin B1 receptor in human IMR90 cells after 60 minsDisplacement of [3H](Des-Arg10)-Kallidin from bradykinin B1 receptor in human IMR90 cells after 60 mins |
ChEMBL | None | None | None | None | 10.1016/j.bmcl.2013.01.025 | ||||
| CHEMBL264100 | 1378 | None | 24 | Human | Binding | pIC50 | = | 9.1 | 9.1 | 6 | 3 | Displacement of [3H](Des-Arg10)-Kallidin from bradykinin B1 receptor in human IMR90 cells after 60 minsDisplacement of [3H](Des-Arg10)-Kallidin from bradykinin B1 receptor in human IMR90 cells after 60 mins |
ChEMBL | None | None | None | None | 10.1016/j.bmcl.2013.01.025 | ||||
| 44579694 | 193252 | None | 0 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | Inhibition of human bradykinin B1 receptorInhibition of human bradykinin B1 receptor |
ChEMBL | 486 | 7 | 3 | 5 | 3.6 | Cc1c(C(=O)NCCC2CCN(C3CCN(C)CC3)CC2)n[nH]c1NC(=O)c1ccccc1Cl | 10.1016/j.bmcl.2008.08.014 | ||
| CHEMBL522947 | 193252 | None | 0 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | Inhibition of human bradykinin B1 receptorInhibition of human bradykinin B1 receptor |
ChEMBL | 486 | 7 | 3 | 5 | 3.6 | Cc1c(C(=O)NCCC2CCN(C3CCN(C)CC3)CC2)n[nH]c1NC(=O)c1ccccc1Cl | 10.1016/j.bmcl.2008.08.014 | ||
| 10031511 | 16953 | None | 0 | Human | Binding | pIC50 | = | 8.7 | 8.7 | 1 | 2 | Compound was tested for inhibition against human bradykinin B1 receptor using FLIPR assayCompound was tested for inhibition against human bradykinin B1 receptor using FLIPR assay |
ChEMBL | 601 | 9 | 2 | 6 | 5.7 | CCCN1C(=O)[C@H](NC(=O)Nc2ccc(N3CCN(c4ccncc4)CC3)cc2)N=C(CCc2ccccc2)c2ccccc21 | 10.1021/jm034020y | ||
| CHEMBL1253497 | 16953 | None | 0 | Human | Binding | pIC50 | = | 8.7 | 8.7 | 1 | 2 | Compound was tested for inhibition against human bradykinin B1 receptor using FLIPR assayCompound was tested for inhibition against human bradykinin B1 receptor using FLIPR assay |
ChEMBL | 601 | 9 | 2 | 6 | 5.7 | CCCN1C(=O)[C@H](NC(=O)Nc2ccc(N3CCN(c4ccncc4)CC3)cc2)N=C(CCc2ccccc2)c2ccccc21 | 10.1021/jm034020y | ||
| 11204003 | 77250 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | Inhibition of human B1 receptorInhibition of human B1 receptor |
ChEMBL | 579 | 7 | 2 | 4 | 6.0 | Cc1ccc(S(=O)(=O)N2CCCC[C@H]2CC(=O)N[C@@H]2CCCc3cc(CNC(C)(C)C)ccc32)cc1C(F)(F)F | 10.1016/j.bmcl.2006.01.069 | ||
| CHEMBL207947 | 77250 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | Inhibition of human B1 receptorInhibition of human B1 receptor |
ChEMBL | 579 | 7 | 2 | 4 | 6.0 | Cc1ccc(S(=O)(=O)N2CCCC[C@H]2CC(=O)N[C@@H]2CCCc3cc(CNC(C)(C)C)ccc32)cc1C(F)(F)F | 10.1016/j.bmcl.2006.01.069 | ||
| 44410020 | 138307 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | Inhibition of human B1 receptorInhibition of human B1 receptor |
ChEMBL | 549 | 7 | 1 | 4 | 5.0 | O=C(C[C@@H]1CCCCN1S(=O)(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCCc2cc(CN3CCC3)ccc21 | 10.1016/j.bmcl.2006.01.069 | ||
| CHEMBL377011 | 138307 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | Inhibition of human B1 receptorInhibition of human B1 receptor |
ChEMBL | 549 | 7 | 1 | 4 | 5.0 | O=C(C[C@@H]1CCCCN1S(=O)(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCCc2cc(CN3CCC3)ccc21 | 10.1016/j.bmcl.2006.01.069 | ||
| 44410316 | 140950 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | Inhibition of human B1 receptorInhibition of human B1 receptor |
ChEMBL | 531 | 7 | 2 | 4 | 5.4 | CC(C)(C)NCc1ccc2c(c1)CCC[C@H]2NC(=O)C[C@@H]1CCCCN1S(=O)(=O)c1cccc(Cl)c1 | 10.1016/j.bmcl.2006.01.069 | ||
| CHEMBL381964 | 140950 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | Inhibition of human B1 receptorInhibition of human B1 receptor |
ChEMBL | 531 | 7 | 2 | 4 | 5.4 | CC(C)(C)NCc1ccc2c(c1)CCC[C@H]2NC(=O)C[C@@H]1CCCCN1S(=O)(=O)c1cccc(Cl)c1 | 10.1016/j.bmcl.2006.01.069 | ||
| 44410269 | 166229 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Inhibition of human B1 receptorInhibition of human B1 receptor |
ChEMBL | 569 | 11 | 2 | 5 | 5.9 | CCCCOc1ccc(S(=O)(=O)N2CCCC[C@H]2CC(=O)N[C@@H]2CCCc3cc(CNC(C)(C)C)ccc32)cc1 | 10.1016/j.bmcl.2006.01.069 | ||
| CHEMBL426130 | 166229 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Inhibition of human B1 receptorInhibition of human B1 receptor |
ChEMBL | 569 | 11 | 2 | 5 | 5.9 | CCCCOc1ccc(S(=O)(=O)N2CCCC[C@H]2CC(=O)N[C@@H]2CCCc3cc(CNC(C)(C)C)ccc32)cc1 | 10.1016/j.bmcl.2006.01.069 | ||
| 11215189 | 168896 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | Inhibition of human B1 receptorInhibition of human B1 receptor |
ChEMBL | 565 | 9 | 2 | 4 | 5.6 | CC(C)CNCc1ccc2c(c1)CCC[C@H]2NC(=O)C[C@@H]1CCCCN1S(=O)(=O)c1cccc(C(F)(F)F)c1 | 10.1016/j.bmcl.2006.01.069 | ||
| CHEMBL437509 | 168896 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | Inhibition of human B1 receptorInhibition of human B1 receptor |
ChEMBL | 565 | 9 | 2 | 4 | 5.6 | CC(C)CNCc1ccc2c(c1)CCC[C@H]2NC(=O)C[C@@H]1CCCCN1S(=O)(=O)c1cccc(C(F)(F)F)c1 | 10.1016/j.bmcl.2006.01.069 | ||
| 11444270 | 76747 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | Inhibition of human B1 receptorInhibition of human B1 receptor |
ChEMBL | 553 | 7 | 2 | 5 | 5.9 | CC(C)(C)NCc1ccc2c(c1)CCC[C@H]2NC(=O)C[C@@H]1CCCCN1S(=O)(=O)c1csc2ccccc12 | 10.1016/j.bmcl.2006.01.069 | ||
| CHEMBL206554 | 76747 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | Inhibition of human B1 receptorInhibition of human B1 receptor |
ChEMBL | 553 | 7 | 2 | 5 | 5.9 | CC(C)(C)NCc1ccc2c(c1)CCC[C@H]2NC(=O)C[C@@H]1CCCCN1S(=O)(=O)c1csc2ccccc12 | 10.1016/j.bmcl.2006.01.069 | ||
| 11444165 | 140966 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | Inhibition of human B1 receptorInhibition of human B1 receptor |
ChEMBL | 545 | 7 | 2 | 4 | 5.7 | Cc1ccc(S(=O)(=O)N2CCCC[C@H]2CC(=O)N[C@@H]2CCCc3cc(CNC(C)(C)C)ccc32)cc1Cl | 10.1016/j.bmcl.2006.01.069 | ||
| CHEMBL381979 | 140966 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | Inhibition of human B1 receptorInhibition of human B1 receptor |
ChEMBL | 545 | 7 | 2 | 4 | 5.7 | Cc1ccc(S(=O)(=O)N2CCCC[C@H]2CC(=O)N[C@@H]2CCCc3cc(CNC(C)(C)C)ccc32)cc1Cl | 10.1016/j.bmcl.2006.01.069 | ||
| 11512379 | 166100 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | Inhibition of human B1 receptorInhibition of human B1 receptor |
ChEMBL | 555 | 7 | 2 | 7 | 4.7 | CC(C)(C)NCc1ccc2c(c1)CCC[C@H]2NC(=O)C[C@@H]1CCCCN1S(=O)(=O)c1cccc2nsnc12 | 10.1016/j.bmcl.2006.01.069 | ||
| CHEMBL425416 | 166100 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | Inhibition of human B1 receptorInhibition of human B1 receptor |
ChEMBL | 555 | 7 | 2 | 7 | 4.7 | CC(C)(C)NCc1ccc2c(c1)CCC[C@H]2NC(=O)C[C@@H]1CCCCN1S(=O)(=O)c1cccc2nsnc12 | 10.1016/j.bmcl.2006.01.069 | ||
| 44410368 | 76789 | None | 0 | Human | Binding | pIC50 | = | 5.8 | 5.8 | - | 0 | Inhibition of human B1 receptorInhibition of human B1 receptor |
ChEMBL | 553 | 7 | 2 | 5 | 4.8 | CC(C)(C)NCc1ccc2c(c1)OCC[C@H]2NC(=O)C[C@@H]1CCCN1S(=O)(=O)c1cccc(C(F)(F)F)c1 | 10.1016/j.bmcl.2006.01.069 | ||
| CHEMBL206801 | 76789 | None | 0 | Human | Binding | pIC50 | = | 5.8 | 5.8 | - | 0 | Inhibition of human B1 receptorInhibition of human B1 receptor |
ChEMBL | 553 | 7 | 2 | 5 | 4.8 | CC(C)(C)NCc1ccc2c(c1)OCC[C@H]2NC(=O)C[C@@H]1CCCN1S(=O)(=O)c1cccc(C(F)(F)F)c1 | 10.1016/j.bmcl.2006.01.069 | ||
| 11203826 | 140209 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | Inhibition of human B1 receptorInhibition of human B1 receptor |
ChEMBL | 563 | 9 | 2 | 4 | 5.3 | O=C(C[C@@H]1CCCCN1S(=O)(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCCc2cc(CNCC3CC3)ccc21 | 10.1016/j.bmcl.2006.01.069 | ||
| CHEMBL380117 | 140209 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | Inhibition of human B1 receptorInhibition of human B1 receptor |
ChEMBL | 563 | 9 | 2 | 4 | 5.3 | O=C(C[C@@H]1CCCCN1S(=O)(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCCc2cc(CNCC3CC3)ccc21 | 10.1016/j.bmcl.2006.01.069 | ||
| 44410026 | 76824 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | Inhibition of human B1 receptorInhibition of human B1 receptor |
ChEMBL | 567 | 7 | 2 | 5 | 5.2 | CC(C)(C)NCc1ccc2c(c1)OCC[C@H]2NC(=O)C[C@@H]1CCCCN1S(=O)(=O)c1cccc(C(F)(F)F)c1 | 10.1016/j.bmcl.2006.01.069 | ||
| CHEMBL206901 | 76824 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | Inhibition of human B1 receptorInhibition of human B1 receptor |
ChEMBL | 567 | 7 | 2 | 5 | 5.2 | CC(C)(C)NCc1ccc2c(c1)OCC[C@H]2NC(=O)C[C@@H]1CCCCN1S(=O)(=O)c1cccc(C(F)(F)F)c1 | 10.1016/j.bmcl.2006.01.069 | ||
| 665 | 973 | None | 2 | Rat | Binding | pIC50 | = | 6.8 | 6.8 | -1023 | 2 | Inhibition of rat bradykinin B1 receptorInhibition of rat bradykinin B1 receptor |
ChEMBL | 585 | 8 | 3 | 6 | 3.6 | O=C(C[C@@H]1C(=O)Nc2c(N1S(=O)(=O)c1ccc(c(c1)Cl)Cl)cccc2)NCCc1ccc(cc1)C1=NCCN1 | 10.1021/jm1000776 | ||
| 9916412 | 973 | None | 2 | Rat | Binding | pIC50 | = | 6.8 | 6.8 | -1023 | 2 | Inhibition of rat bradykinin B1 receptorInhibition of rat bradykinin B1 receptor |
ChEMBL | 585 | 8 | 3 | 6 | 3.6 | O=C(C[C@@H]1C(=O)Nc2c(N1S(=O)(=O)c1ccc(c(c1)Cl)Cl)cccc2)NCCc1ccc(cc1)C1=NCCN1 | 10.1021/jm1000776 | ||
| CHEMBL189123 | 973 | None | 2 | Rat | Binding | pIC50 | = | 6.8 | 6.8 | -1023 | 2 | Inhibition of rat bradykinin B1 receptorInhibition of rat bradykinin B1 receptor |
ChEMBL | 585 | 8 | 3 | 6 | 3.6 | O=C(C[C@@H]1C(=O)Nc2c(N1S(=O)(=O)c1ccc(c(c1)Cl)Cl)cccc2)NCCc1ccc(cc1)C1=NCCN1 | 10.1021/jm1000776 | ||
| 10187347 | 193469 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 1 | Compound was tested for inhibition against human bradykinin B1 receptor using FLIPR assayCompound was tested for inhibition against human bradykinin B1 receptor using FLIPR assay |
ChEMBL | 544 | 7 | 2 | 5 | 5.5 | CCCN1C(=O)C(NC(=O)Nc2ccc(N3CCC(N(C)C)CC3)cc2)N=C(C2CCCCC2)c2ccccc21 | 10.1021/jm034020y | ||
| CHEMBL52498 | 193469 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 1 | Compound was tested for inhibition against human bradykinin B1 receptor using FLIPR assayCompound was tested for inhibition against human bradykinin B1 receptor using FLIPR assay |
ChEMBL | 544 | 7 | 2 | 5 | 5.5 | CCCN1C(=O)C(NC(=O)Nc2ccc(N3CCC(N(C)C)CC3)cc2)N=C(C2CCCCC2)c2ccccc21 | 10.1021/jm034020y | ||
| 44410143 | 77365 | None | 0 | Human | Binding | pIC50 | = | 5.8 | 5.8 | - | 0 | Inhibition of human B1 receptorInhibition of human B1 receptor |
ChEMBL | 497 | 7 | 2 | 4 | 4.7 | CC(C)(C)NCc1ccc2c(c1)CCC[C@H]2NC(=O)C[C@@H]1CCCCN1S(=O)(=O)c1ccccc1 | 10.1016/j.bmcl.2006.01.069 | ||
| CHEMBL208386 | 77365 | None | 0 | Human | Binding | pIC50 | = | 5.8 | 5.8 | - | 0 | Inhibition of human B1 receptorInhibition of human B1 receptor |
ChEMBL | 497 | 7 | 2 | 4 | 4.7 | CC(C)(C)NCc1ccc2c(c1)CCC[C@H]2NC(=O)C[C@@H]1CCCCN1S(=O)(=O)c1ccccc1 | 10.1016/j.bmcl.2006.01.069 | ||
| 44410084 | 76958 | None | 0 | Human | Binding | pIC50 | = | 5.7 | 5.7 | - | 0 | Inhibition of human B1 receptorInhibition of human B1 receptor |
ChEMBL | 591 | 8 | 2 | 4 | 5.5 | O=C(C[C@@H]1CCCCN1S(=O)(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCCc2cc(CNCC(F)(F)F)ccc21 | 10.1016/j.bmcl.2006.01.069 | ||
| CHEMBL207033 | 76958 | None | 0 | Human | Binding | pIC50 | = | 5.7 | 5.7 | - | 0 | Inhibition of human B1 receptorInhibition of human B1 receptor |
ChEMBL | 591 | 8 | 2 | 4 | 5.5 | O=C(C[C@@H]1CCCCN1S(=O)(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCCc2cc(CNCC(F)(F)F)ccc21 | 10.1016/j.bmcl.2006.01.069 | ||
| 10031511 | 16953 | None | 0 | Rat | Binding | pIC50 | = | 8.6 | 8.6 | -1 | 2 | Compound was tested for inhibition against rat Bradykinin receptor B1 using FLIPR assayCompound was tested for inhibition against rat Bradykinin receptor B1 using FLIPR assay |
ChEMBL | 601 | 9 | 2 | 6 | 5.7 | CCCN1C(=O)[C@H](NC(=O)Nc2ccc(N3CCN(c4ccncc4)CC3)cc2)N=C(CCc2ccccc2)c2ccccc21 | 10.1021/jm034020y | ||
| CHEMBL1253497 | 16953 | None | 0 | Rat | Binding | pIC50 | = | 8.6 | 8.6 | -1 | 2 | Compound was tested for inhibition against rat Bradykinin receptor B1 using FLIPR assayCompound was tested for inhibition against rat Bradykinin receptor B1 using FLIPR assay |
ChEMBL | 601 | 9 | 2 | 6 | 5.7 | CCCN1C(=O)[C@H](NC(=O)Nc2ccc(N3CCN(c4ccncc4)CC3)cc2)N=C(CCc2ccccc2)c2ccccc21 | 10.1021/jm034020y | ||
| 10031511 | 16953 | None | 0 | Rat | Binding | pIC50 | = | 8.6 | 8.6 | -1 | 2 | Inhibition of rat bradykinin B1 receptorInhibition of rat bradykinin B1 receptor |
ChEMBL | 601 | 9 | 2 | 6 | 5.7 | CCCN1C(=O)[C@H](NC(=O)Nc2ccc(N3CCN(c4ccncc4)CC3)cc2)N=C(CCc2ccccc2)c2ccccc21 | 10.1021/jm1000776 | ||
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