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Assay Detail

CHEMBL656133

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Functional
Antagonistic activity against Bradykinin receptor B1 of rat ileum longitudinal smooth muscle.
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Ileum
Confidence 8 — Homologous single protein target
Curated By Expert

Target

B1 bradykinin receptor (CHEMBL4613)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

A new class of pseudopeptide antagonists of the kinin B1 receptor containing alkyl spacers.
Galoppini C, Meini S, Tancredi M, Di Fenza A, Triolo A, Quartara L, Maggi CA, Formaggio F, Toniolo C, Mazzucco S, Papini A, Rovero P.
J Med Chem (1999) 42 : 409 -414
PubMed 9986712 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 22 6.20 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2370700 1 8.10
CHEMBL2370699 1 7.70
CHEMBL410363 1 7.20
CHEMBL424272 1 7.10
CHEMBL339159 1 7.00
CHEMBL264517 1 7.00
CHEMBL1793829 1 6.80
CHEMBL130222 1 6.60
CHEMBL265814 1 6.30
CHEMBL337833 1 6.30
CHEMBL385081 1 6.10
CHEMBL334538 1 6.00
CHEMBL339389 1 5.90
CHEMBL134135 1 5.70
CHEMBL405644 1 5.70
CHEMBL266975 1 5.60
CHEMBL131647 1 5.50
CHEMBL335247 1 5.40
CHEMBL218454 1 5.20
CHEMBL133164 1 5.20
CHEMBL384846 1 5.00
CHEMBL133560 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2370700 Kd = 7.943 nM 8.10
CHEMBL2370699 Kd = 19.95 nM 7.70
CHEMBL410363 Kd = 63.1 nM 7.20
CHEMBL424272 Kd = 79.43 nM 7.10
CHEMBL339159 Kd = 100.0 nM 7.00
CHEMBL264517 Kd = 100.0 nM 7.00
CHEMBL1793829 Kd = 158.49 nM 6.80
CHEMBL130222 Kd = 251.19 nM 6.60
CHEMBL265814 Kd = 501.19 nM 6.30
CHEMBL337833 Kd = 501.19 nM 6.30
CHEMBL385081 Kd = 794.33 nM 6.10
CHEMBL334538 Kd = 1000.0 nM 6.00
CHEMBL339389 Kd = 1258.93 nM 5.90
CHEMBL134135 Kd = 1995.26 nM 5.70
CHEMBL405644 Kd = 1995.26 nM 5.70
CHEMBL266975 Kd = 2511.89 nM 5.60
CHEMBL131647 Kd = 3162.28 nM 5.50
CHEMBL335247 Kd = 3981.07 nM 5.40
CHEMBL218454 Kd = 6309.57 nM 5.20
CHEMBL133164 Kd = 6309.57 nM 5.20
CHEMBL384846 Kd = 10000.0 nM 5.00
CHEMBL133560 Kd = 10000.0 nM 5.00