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Assay Detail

CHEMBL652382

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

Binding
Inhibition of binding of [3H]BK to rat bradykinin B2 receptor expressed in NG108-15 neuroblastoma-glioma hybrid cell membranes
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

B2 bradykinin receptor (CHEMBL2501)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

1-(2-Nitrophenyl)thiosemicarbazides: a novel class of potent, orally active non-peptide antagonist for the bradykinin B(2) receptor.
Dziadulewicz EK, Ritchie TJ, Hallett A, Snell CR, Ko SY, Wrigglesworth R, Hughes GA, Dunstan AR, Bloomfield GC, Drake GS, Brown MC, Lee W, Burgess GM, Davis C, Yaqoob M, Perkins MN, Campbell EA, Davis AJ, Rang HP.
J Med Chem (2000) 43 : 769 -771
PubMed 10715143 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.06 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2112937 1 9.30
CHEMBL2112044 1 9.22
CHEMBL349817 1 8.74
CHEMBL165627 1 8.40
CHEMBL164636 1 7.42
CHEMBL164754 1 6.83
CHEMBL164848 1 6.51
CHEMBL352459 1 6.27
CHEMBL163956 1 5.80
CHEMBL165240 1 5.15
CHEMBL164968 1 4.00
CHEMBL164551 1 -
CHEMBL165238 1 -
CHEMBL163840 1 -
CHEMBL350109 1 -
CHEMBL164914 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2112937 Ki = 0.5 nM 9.30
CHEMBL2112044 Ki = 0.6 nM 9.22
CHEMBL349817 Ki = 1.8 nM 8.74
CHEMBL165627 Ki = 4.0 nM 8.40
CHEMBL164636 Ki = 38.0 nM 7.42
CHEMBL164754 Ki = 148.0 nM 6.83
CHEMBL164848 Ki = 310.0 nM 6.51
CHEMBL352459 Ki = 540.0 nM 6.27
CHEMBL163956 Ki = 1600.0 nM 5.80
CHEMBL165240 Ki = 7100.0 nM 5.15
CHEMBL164968 Ki = 100000.0 nM 4.00
CHEMBL164551 Ki > 100000.0 nM -
CHEMBL165238 Ki > 100000.0 nM -
CHEMBL163840 Ki > 100000.0 nM -
CHEMBL350109 Ki > 100000.0 nM -
CHEMBL164914 Ki > 100000.0 nM -