Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL818749

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of specific binding of [3H]BK to bradykinin B2 receptors of guinea pig ileum (GPI)
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Ileum
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

B2 bradykinin receptor (CHEMBL4111)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Novel series of O-substituted 8-quinolines and 4-benzothiazoles as potent antagonists of the bradykinin B2 receptors.
Heitsch H, Wagner A, Schölkens BA, Wirth K.
Bioorg Med Chem Lett (1999) 9 : 327 -332
PubMed 10091678 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 8.44 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL113169 1 10.00
CHEMBL113963 1 10.00
CHEMBL325255 1 9.52
CHEMBL115163 1 9.22
CHEMBL112140 1 8.89
CHEMBL323693 1 8.89
CHEMBL114732 1 8.89
CHEMBL114401 1 8.74
CHEMBL113465 1 8.60
CHEMBL112991 1 8.55
CHEMBL324950 1 8.54
CHEMBL113222 1 8.51
CHEMBL333832 1 8.47
CHEMBL324575 1 8.41
CHEMBL325601 1 8.27
CHEMBL113502 1 8.22
CHEMBL114915 1 8.20
CHEMBL114180 1 8.08
CHEMBL325742 1 8.04
CHEMBL112360 1 8.04
CHEMBL113176 1 7.34
CHEMBL325624 1 6.80
CHEMBL113320 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL113169 Ki = 0.1 nM 10.00
CHEMBL113963 Ki = 0.1 nM 10.00
CHEMBL325255 Ki = 0.3 nM 9.52
CHEMBL115163 Ki = 0.6 nM 9.22
CHEMBL112140 Ki = 1.3 nM 8.89
CHEMBL323693 Ki = 1.3 nM 8.89
CHEMBL114732 Ki = 1.3 nM 8.89
CHEMBL114401 Ki = 1.8 nM 8.74
CHEMBL113465 Ki = 2.5 nM 8.60
CHEMBL112991 Ki = 2.8 nM 8.55
CHEMBL324950 Ki = 2.9 nM 8.54
CHEMBL113222 Ki = 3.1 nM 8.51
CHEMBL333832 Ki = 3.4 nM 8.47
CHEMBL324575 Ki = 3.9 nM 8.41
CHEMBL325601 Ki = 5.4 nM 8.27
CHEMBL113502 Ki = 6.0 nM 8.22
CHEMBL114915 Ki = 6.3 nM 8.20
CHEMBL114180 Ki = 8.3 nM 8.08
CHEMBL325742 Ki = 9.1 nM 8.04
CHEMBL112360 Ki = 9.2 nM 8.04
CHEMBL113176 Ki = 45.4 nM 7.34
CHEMBL325624 Ki = 160.0 nM 6.80
CHEMBL113320 Ki = 1300.0 nM 5.89