Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL617075

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

Binding
Binding affinity for displacement of [3H]ketanserin to human 5-hydroxytryptamine 2A receptor stably expressed in CHO cells
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 2A (CHEMBL224)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

4-(Phenylsulfonyl)piperidines: novel, selective, and bioavailable 5-HT(2A) receptor antagonists.
Fletcher SR, Burkamp F, Blurton P, Cheng SK, Clarkson R, O'Connor D, Spinks D, Tudge M, van Niel MB, Patel S, Chapman K, Marwood R, Shepheard S, Bentley G, Cook GP, Bristow LJ, Castro JL, Hutson PH, MacLeod AM.
J Med Chem (2002) 45 : 492 -503
PubMed 11784153 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 8.53 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL83894 FANANSERIN 2.0 1 10.40
CHEMBL504699 1 10.22
CHEMBL74355 VOLINANSERIN 3.0 1 9.51
CHEMBL145939 1 9.48
CHEMBL357807 1 9.44
CHEMBL146144 1 9.40
CHEMBL146595 1 9.39
CHEMBL358075 1 9.38
CHEMBL146485 1 9.30
CHEMBL148058 1 9.28
CHEMBL146998 1 9.28
CHEMBL147048 1 9.18
CHEMBL148280 1 8.92
CHEMBL149429 1 8.85
CHEMBL146233 1 8.74
CHEMBL147431 1 8.62
CHEMBL146620 1 8.62
CHEMBL150220 1 8.59
CHEMBL150210 1 8.54
CHEMBL148348 1 8.51
CHEMBL149423 1 8.48
CHEMBL147164 1 8.30
CHEMBL343411 1 7.82
CHEMBL148565 1 7.82
CHEMBL359270 1 7.80
CHEMBL148418 1 7.80
CHEMBL122761 1 7.80
CHEMBL149510 1 7.51
CHEMBL423206 1 7.02
CHEMBL148103 1 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL83894 FANANSERIN Ki = 0.04 nM 10.40
CHEMBL504699 Ki = 0.06 nM 10.22
CHEMBL74355 VOLINANSERIN Ki = 0.31 nM 9.51
CHEMBL145939 Ki = 0.33 nM 9.48
CHEMBL357807 Ki = 0.36 nM 9.44
CHEMBL146144 Ki = 0.4 nM 9.40
CHEMBL146595 Ki = 0.41 nM 9.39
CHEMBL358075 Ki = 0.42 nM 9.38
CHEMBL146485 Ki = 0.5 nM 9.30
CHEMBL148058 Ki = 0.52 nM 9.28
CHEMBL146998 Ki = 0.53 nM 9.28
CHEMBL147048 Ki = 0.66 nM 9.18
CHEMBL148280 Ki = 1.2 nM 8.92
CHEMBL149429 Ki = 1.4 nM 8.85
CHEMBL146233 Ki = 1.8 nM 8.74
CHEMBL146620 Ki = 2.4 nM 8.62
CHEMBL147431 Ki = 2.4 nM 8.62
CHEMBL150220 Ki = 2.6 nM 8.59
CHEMBL150210 Ki = 2.9 nM 8.54
CHEMBL148348 Ki = 3.1 nM 8.51
CHEMBL149423 Ki = 3.3 nM 8.48
CHEMBL147164 Ki = 5.0 nM 8.30
CHEMBL343411 Ki = 15.0 nM 7.82
CHEMBL148565 Ki = 15.0 nM 7.82
CHEMBL359270 Ki = 16.0 nM 7.80
CHEMBL122761 Ki = 16.0 nM 7.80
CHEMBL148418 Ki = 16.0 nM 7.80
CHEMBL149510 Ki = 31.0 nM 7.51
CHEMBL423206 Ki = 95.0 nM 7.02
CHEMBL148103 Ki = 150.0 nM 6.82
CHEMBL358839 Ki = 630.0 nM 6.20
CHEMBL357883 Ki = 970.0 nM 6.01
CHEMBL146448 Ki > 2000.0 nM -