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Assay Detail

CHEMBL656501

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

Binding
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 ↗
58
Total Activities
58
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

A novel class of orally active non-peptide bradykinin B2 receptor antagonists. 3. Discovering bioisosteres of the imidazo[1,2-a] pyridine moiety.
Abe Y, Kayakiri H, Satoh S, Inoue T, Sawada Y, Inamura N, Asano M, Aramori I, Hatori C, Sawai H, Oku T, Tanaka H.
J Med Chem (1998) 41 : 4062 -4079
PubMed 9767643 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 58 8.35 10.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2028850 ICATIBANT 4.0 1 10.05
CHEMBL553614 — — 1 9.89
CHEMBL130517 FR-173657 — 1 9.34
CHEMBL552543 — — 1 9.33
CHEMBL538732 — — 1 9.30
CHEMBL544599 — — 1 9.30
CHEMBL542096 — — 1 9.29
CHEMBL553293 — — 1 9.26
CHEMBL540819 — — 1 9.21
CHEMBL264751 — — 1 9.19
CHEMBL543899 — — 1 9.18
CHEMBL542232 — — 1 9.17
CHEMBL544601 — — 1 9.16
CHEMBL130436 — — 1 9.12
CHEMBL542958 — — 1 9.10
CHEMBL553843 — — 1 9.09
CHEMBL44557 — — 1 9.08
CHEMBL132860 — — 1 9.03
CHEMBL132510 — — 1 9.03
CHEMBL543781 — — 1 9.01
CHEMBL554206 — — 1 9.00
CHEMBL131263 — — 1 8.96
CHEMBL130782 — — 1 8.96
CHEMBL539294 — — 1 8.96
CHEMBL552986 — — 1 8.89
CHEMBL542479 — — 1 8.85
CHEMBL44087 — — 1 8.80
CHEMBL335946 — — 1 8.72
CHEMBL541590 — — 1 8.66
CHEMBL555465 — — 1 8.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2028850 ICATIBANT IC50 = 0.09 nM 10.05
CHEMBL553614 — IC50 = 0.13 nM 9.89
CHEMBL130517 FR-173657 IC50 = 0.46 nM 9.34
CHEMBL552543 — IC50 = 0.47 nM 9.33
CHEMBL538732 — IC50 = 0.5 nM 9.30
CHEMBL544599 — IC50 = 0.5 nM 9.30
CHEMBL542096 — IC50 = 0.51 nM 9.29
CHEMBL553293 — IC50 = 0.55 nM 9.26
CHEMBL540819 — IC50 = 0.62 nM 9.21
CHEMBL264751 — IC50 = 0.65 nM 9.19
CHEMBL543899 — IC50 = 0.66 nM 9.18
CHEMBL542232 — IC50 = 0.68 nM 9.17
CHEMBL544601 — IC50 = 0.69 nM 9.16
CHEMBL130436 — IC50 = 0.76 nM 9.12
CHEMBL542958 — IC50 = 0.79 nM 9.10
CHEMBL553843 — IC50 = 0.82 nM 9.09
CHEMBL44557 — IC50 = 0.83 nM 9.08
CHEMBL132860 — IC50 = 0.94 nM 9.03
CHEMBL132510 — IC50 = 0.94 nM 9.03
CHEMBL543781 — IC50 = 0.97 nM 9.01
CHEMBL554206 — IC50 = 1.0 nM 9.00
CHEMBL131263 — IC50 = 1.1 nM 8.96
CHEMBL130782 — IC50 = 1.1 nM 8.96
CHEMBL539294 — IC50 = 1.1 nM 8.96
CHEMBL552986 — IC50 = 1.3 nM 8.89
CHEMBL542479 — IC50 = 1.4 nM 8.85
CHEMBL44087 — IC50 = 1.6 nM 8.80
CHEMBL335946 — IC50 = 1.9 nM 8.72
CHEMBL541590 — IC50 = 2.2 nM 8.66
CHEMBL555465 — IC50 = 2.4 nM 8.62
CHEMBL133339 — IC50 = 2.4 nM 8.62
CHEMBL555202 — IC50 = 3.3 nM 8.48
CHEMBL133913 — IC50 = 3.5 nM 8.46
CHEMBL334753 — IC50 = 4.1 nM 8.39
CHEMBL133005 — IC50 = 6.3 nM 8.20
CHEMBL542836 — IC50 = 8.7 nM 8.06
CHEMBL43746 — IC50 = 8.9 nM 8.05
CHEMBL288603 — IC50 = 9.1 nM 8.04
CHEMBL295428 — IC50 = 9.5 nM 8.02
CHEMBL336574 — IC50 = 11.0 nM 7.96
CHEMBL543659 — IC50 = 15.0 nM 7.82
CHEMBL334421 — IC50 = 18.0 nM 7.75
CHEMBL41446 — IC50 = 23.0 nM 7.64
CHEMBL240875 — IC50 = 38.0 nM 7.42
CHEMBL424268 — IC50 = 48.0 nM 7.32
CHEMBL296865 — IC50 = 90.0 nM 7.05
CHEMBL288079 — IC50 = 94.0 nM 7.03
CHEMBL298463 — IC50 = 110.0 nM 6.96
CHEMBL290431 — IC50 = 170.0 nM 6.77
CHEMBL295005 — IC50 = 200.0 nM 6.70