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Assay Detail

CHEMBL815924

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

Binding
Inhibitory binding activity against TXA2 receptor in human platelet membrane, using [3H]-SQ 29548 as the radioligand
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Thromboxane A2 receptor (CHEMBL2069)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Interphenylene 7-oxabicyclo[2.2.1]heptane oxazoles. Highly potent, selective, and long-acting thromboxane A2 receptor antagonists.
Misra RN, Brown BR, Sher PM, Patel MM, Hall SE, Han WC, Barrish JC, Kocy O, Harris DN, Goldenberg HJ.
J Med Chem (1993) 36 : 1401 -1417
PubMed 8496908 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 39 8.52 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL31146 1 10.30
CHEMBL31765 1 10.00
CHEMBL30743 1 9.70
CHEMBL30615 1 9.70
CHEMBL281959 1 9.52
CHEMBL283923 1 9.52
CHEMBL29429 1 9.30
CHEMBL30972 1 9.22
CHEMBL410732 1 9.15
CHEMBL31922 1 9.15
CHEMBL281726 1 9.10
CHEMBL31154 1 9.07
CHEMBL286978 1 9.00
CHEMBL285596 1 8.92
CHEMBL278159 1 8.89
CHEMBL30398 1 8.80
CHEMBL31850 1 8.54
CHEMBL287068 1 8.54
CHEMBL30832 1 8.49
CHEMBL30537 1 8.41
CHEMBL283100 BMS-180291 1 8.40
CHEMBL31334 1 8.35
CHEMBL416943 1 8.33
CHEMBL281293 1 8.32
CHEMBL418585 1 8.24
CHEMBL433435 1 8.00
CHEMBL416395 1 7.97
CHEMBL418583 1 7.96
CHEMBL280786 1 7.79
CHEMBL286708 1 7.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL31146 Kd = 0.05 nM 10.30
CHEMBL31765 Kd = 0.1 nM 10.00
CHEMBL30615 Kd = 0.2 nM 9.70
CHEMBL30743 Kd = 0.2 nM 9.70
CHEMBL281959 Kd = 0.3 nM 9.52
CHEMBL283923 Kd = 0.3 nM 9.52
CHEMBL29429 Kd = 0.5 nM 9.30
CHEMBL30972 Kd = 0.6 nM 9.22
CHEMBL410732 Kd = 0.7 nM 9.15
CHEMBL31922 Kd = 0.7 nM 9.15
CHEMBL281726 Kd = 0.8 nM 9.10
CHEMBL31154 Kd = 0.85 nM 9.07
CHEMBL286978 Kd = 1.0 nM 9.00
CHEMBL285596 Kd = 1.2 nM 8.92
CHEMBL278159 Kd = 1.3 nM 8.89
CHEMBL30398 Kd = 1.6 nM 8.80
CHEMBL31850 Kd = 2.9 nM 8.54
CHEMBL287068 Kd = 2.9 nM 8.54
CHEMBL30832 Kd = 3.2 nM 8.49
CHEMBL30537 Kd = 3.9 nM 8.41
CHEMBL283100 BMS-180291 Kd = 4.0 nM 8.40
CHEMBL31334 Kd = 4.5 nM 8.35
CHEMBL416943 Kd = 4.7 nM 8.33
CHEMBL281293 Kd = 4.8 nM 8.32
CHEMBL418585 Kd = 5.8 nM 8.24
CHEMBL433435 Kd = 10.0 nM 8.00
CHEMBL416395 Kd = 10.6 nM 7.97
CHEMBL418583 Kd = 11.0 nM 7.96
CHEMBL280786 Kd = 16.3 nM 7.79
CHEMBL286708 Kd = 18.4 nM 7.74
CHEMBL31043 Kd = 19.0 nM 7.72
CHEMBL287421 Kd = 19.0 nM 7.72
CHEMBL30727 Kd = 20.0 nM 7.70
CHEMBL30377 Kd = 22.0 nM 7.66
CHEMBL2368531 Kd = 22.0 nM 7.66
CHEMBL29947 Kd = 26.0 nM 7.58
CHEMBL282186 Kd = 36.0 nM 7.44
CHEMBL33621 Kd = 45.0 nM 7.35
CHEMBL282601 Kd = 112.0 nM 6.95