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Assay Detail

CHEMBL768491

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

Binding
Binding potency against Platelet activating factor (PAF) receptor using [3H]C18-PAF as radioligand on rabbit platelet membranes
ChEMBL ↗
88
Total Activities
88
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Platelet-activating factor receptor (CHEMBL5136) ↗
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Discovery and evaluation of a series of 3-acylindole imidazopyridine platelet-activating factor antagonists.
Curtin ML, Davidsen SK, Heyman HR, Garland RB, Sheppard GS, Florjancic AS, Xu L, Carrera GM, Steinman DH, Trautmann JA, Albert DH, Magoc TJ, Tapang P, Rhein DA, Conway RG, Luo G, Denissen JF, Marsh KC, Morgan DW, Summers JB.
J Med Chem (1998) 41 : 74 -95
PubMed 9438024 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 88 8.27 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL174592 — — 1 9.82
CHEMBL368113 — — 1 9.72
CHEMBL424947 — — 1 9.29
CHEMBL433795 — — 1 9.20
CHEMBL172859 — — 1 9.20
CHEMBL369233 — — 1 9.17
CHEMBL369854 — — 1 9.11
CHEMBL367398 — — 1 9.09
CHEMBL367085 — — 1 9.07
CHEMBL427307 — — 1 9.07
CHEMBL176797 — — 1 9.06
CHEMBL173584 — — 1 9.05
CHEMBL174198 — — 1 9.04
CHEMBL366553 — — 1 9.04
CHEMBL367922 — — 1 9.02
CHEMBL369225 — — 1 9.00
CHEMBL173586 — — 1 8.96
CHEMBL174668 — — 1 8.92
CHEMBL367964 — — 1 8.89
CHEMBL173122 — — 1 8.89
CHEMBL172819 — — 1 8.89
CHEMBL366508 — — 1 8.85
CHEMBL369395 — — 1 8.82
CHEMBL366998 — — 1 8.82
CHEMBL173497 — — 1 8.82
CHEMBL425688 — — 1 8.77
CHEMBL354819 — — 1 8.74
CHEMBL369614 — — 1 8.70
CHEMBL174402 — — 1 8.70
CHEMBL172484 — — 1 8.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL174592 — Ki = 0.15 nM 9.82
CHEMBL368113 — Ki = 0.19 nM 9.72
CHEMBL424947 — Ki = 0.51 nM 9.29
CHEMBL433795 — Ki = 0.63 nM 9.20
CHEMBL172859 — Ki = 0.63 nM 9.20
CHEMBL369233 — Ki = 0.67 nM 9.17
CHEMBL369854 — Ki = 0.78 nM 9.11
CHEMBL367398 — Ki = 0.82 nM 9.09
CHEMBL367085 — Ki = 0.85 nM 9.07
CHEMBL427307 — Ki = 0.86 nM 9.07
CHEMBL176797 — Ki = 0.87 nM 9.06
CHEMBL173584 — Ki = 0.9 nM 9.05
CHEMBL174198 — Ki = 0.92 nM 9.04
CHEMBL366553 — Ki = 0.91 nM 9.04
CHEMBL367922 — Ki = 0.95 nM 9.02
CHEMBL369225 — Ki = 1.0 nM 9.00
CHEMBL173586 — Ki = 1.1 nM 8.96
CHEMBL174668 — Ki = 1.2 nM 8.92
CHEMBL367964 — Ki = 1.3 nM 8.89
CHEMBL173122 — Ki = 1.3 nM 8.89
CHEMBL172819 — Ki = 1.3 nM 8.89
CHEMBL366508 — Ki = 1.4 nM 8.85
CHEMBL369395 — Ki = 1.5 nM 8.82
CHEMBL366998 — Ki = 1.5 nM 8.82
CHEMBL173497 — Ki = 1.5 nM 8.82
CHEMBL425688 — Ki = 1.7 nM 8.77
CHEMBL354819 — Ki = 1.8 nM 8.74
CHEMBL369614 — Ki = 2.0 nM 8.70
CHEMBL174402 — Ki = 2.0 nM 8.70
CHEMBL172484 — Ki = 2.0 nM 8.70
CHEMBL174859 — Ki = 2.2 nM 8.66
CHEMBL176725 — Ki = 2.3 nM 8.64
CHEMBL368185 — Ki = 2.4 nM 8.62
CHEMBL173642 — Ki = 2.5 nM 8.60
CHEMBL368923 — Ki = 2.9 nM 8.54
CHEMBL369643 — Ki = 2.9 nM 8.54
CHEMBL173191 — Ki = 2.9 nM 8.54
CHEMBL367418 — Ki = 3.2 nM 8.49
CHEMBL174550 — Ki = 3.4 nM 8.47
CHEMBL174104 — Ki = 3.6 nM 8.44
CHEMBL170398 — Ki = 4.0 nM 8.40
CHEMBL368162 — Ki = 4.3 nM 8.37
CHEMBL369578 — Ki = 4.4 nM 8.36
CHEMBL173157 — Ki = 4.7 nM 8.33
CHEMBL367393 — Ki = 5.0 nM 8.30
CHEMBL367295 — Ki = 5.1 nM 8.29
CHEMBL174479 — Ki = 5.2 nM 8.28
CHEMBL172697 — Ki = 5.4 nM 8.27
CHEMBL174262 — Ki = 6.0 nM 8.22
CHEMBL435115 — Ki = 6.1 nM 8.21