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Assay Detail

CHEMBL855749

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

Binding
Displacement of [3H]BK from human bradykinin B2 receptor transfected in CHO cells
ChEMBL ↗
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

B2 bradykinin receptor (CHEMBL3157) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of novel sulfonamide-containing bradykinin hB2 receptor antagonists. 2. Synthesis and structure-activity relationships of alpha,alpha-cycloalkylglycine sulfonamides.
Fattori D, Rossi C, Fincham CI, Caciagli V, Catrambone F, D'Andrea P, Felicetti P, Gensini M, Marastoni E, Nannicini R, Paris M, Terracciano R, Bressan A, Giuliani S, Maggi CA, Meini S, Valenti C, Quartara L.
J Med Chem (2007) 50 : 550 -565
PubMed 17266207 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 34 9.51 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL415366 — — 1 10.30
CHEMBL387452 — — 1 10.30
CHEMBL218427 FASITIBANT 2.0 1 10.30
CHEMBL373607 — — 1 10.10
CHEMBL221285 — — 1 10.00
CHEMBL375354 — — 1 9.90
CHEMBL220478 — — 1 9.90
CHEMBL218636 — — 1 9.80
CHEMBL415151 — — 1 9.70
CHEMBL374272 — — 1 9.70
CHEMBL374224 — — 1 9.70
CHEMBL218540 — — 1 9.70
CHEMBL386794 — — 1 9.60
CHEMBL373459 — — 1 9.60
CHEMBL220591 — — 1 9.50
CHEMBL376866 — — 1 9.50
CHEMBL380273 — — 1 9.40
CHEMBL266493 — — 1 9.40
CHEMBL207939 — — 1 9.40
CHEMBL415152 — — 1 9.40
CHEMBL221683 — — 1 9.40
CHEMBL222167 — — 1 9.30
CHEMBL220693 — — 1 9.30
CHEMBL375576 — — 1 9.20
CHEMBL249235 — — 1 9.20
CHEMBL374273 — — 1 9.20
CHEMBL220596 — — 1 9.20
CHEMBL375820 — — 1 9.20
CHEMBL205093 — — 1 9.20
CHEMBL383167 — — 1 9.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL415366 — Ki = 0.05012 nM 10.30
CHEMBL387452 — Ki = 0.05012 nM 10.30
CHEMBL218427 FASITIBANT Ki = 0.05012 nM 10.30
CHEMBL373607 — Ki = 0.07943 nM 10.10
CHEMBL221285 — Ki = 0.1 nM 10.00
CHEMBL375354 — Ki = 0.1259 nM 9.90
CHEMBL220478 — Ki = 0.1259 nM 9.90
CHEMBL218636 — Ki = 0.1585 nM 9.80
CHEMBL374272 — Ki = 0.1995 nM 9.70
CHEMBL218540 — Ki = 0.1995 nM 9.70
CHEMBL374224 — Ki = 0.1995 nM 9.70
CHEMBL415151 — Ki = 0.1995 nM 9.70
CHEMBL386794 — Ki = 0.2512 nM 9.60
CHEMBL373459 — Ki = 0.2512 nM 9.60
CHEMBL376866 — Ki = 0.3162 nM 9.50
CHEMBL220591 — Ki = 0.3162 nM 9.50
CHEMBL266493 — Ki = 0.3981 nM 9.40
CHEMBL221683 — Ki = 0.3981 nM 9.40
CHEMBL415152 — Ki = 0.3981 nM 9.40
CHEMBL207939 — Ki = 0.3981 nM 9.40
CHEMBL380273 — Ki = 0.3981 nM 9.40
CHEMBL222167 — Ki = 0.5012 nM 9.30
CHEMBL220693 — Ki = 0.5012 nM 9.30
CHEMBL375576 — Ki = 0.631 nM 9.20
CHEMBL249235 — Ki = 0.631 nM 9.20
CHEMBL374273 — Ki = 0.631 nM 9.20
CHEMBL220596 — Ki = 0.631 nM 9.20
CHEMBL375820 — Ki = 0.631 nM 9.20
CHEMBL205093 — Ki = 0.631 nM 9.20
CHEMBL383167 — Ki = 0.631 nM 9.20
CHEMBL267493 — Ki = 0.7943 nM 9.10
CHEMBL375689 — Ki = 1.0 nM 9.00
CHEMBL222156 — Ki = 1.259 nM 8.90
CHEMBL220595 — Ki = 1.585 nM 8.80