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Assay Detail

CHEMBL617063

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

Binding
Ability to displace [3H]ketanserin binding to human 5-hydroxytryptamine 2A receptor stably expressed in CHO cells
31
Total Activities
31
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

3-(4-Fluoropiperidin-3-yl)-2-phenylindoles as high affinity, selective, and orally bioavailable h5-HT(2A) receptor antagonists.
Rowley M, Hallett DJ, Goodacre S, Moyes C, Crawforth J, Sparey TJ, Patel S, Marwood R, Patel S, Thomas S, Hitzel L, O'Connor D, Szeto N, Castro JL, Hutson PH, MacLeod AM.
J Med Chem (2001) 44 : 1603 -1614
PubMed 11334570 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 31 8.67 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL504699 1 10.22
CHEMBL497064 1 10.05
CHEMBL296512 1 10.05
CHEMBL497054 1 9.96
CHEMBL523245 1 9.92
CHEMBL496860 1 9.64
CHEMBL507898 1 9.60
CHEMBL496687 1 9.47
CHEMBL523760 1 9.46
CHEMBL497877 1 9.37
CHEMBL498729 1 9.34
CHEMBL40584 1 9.32
CHEMBL2368734 1 9.27
CHEMBL523585 1 9.16
CHEMBL42557 1 9.00
CHEMBL2113667 1 8.92
CHEMBL498048 1 8.64
CHEMBL2368748 1 8.48
CHEMBL497878 1 8.40
CHEMBL43819 1 8.33
CHEMBL496852 1 7.99
CHEMBL507727 1 7.98
CHEMBL295559 1 7.92
CHEMBL43697 1 7.85
CHEMBL40284 1 7.75
CHEMBL46523 1 7.70
CHEMBL295596 1 7.58
CHEMBL44310 1 7.23
CHEMBL2368745 1 7.16
CHEMBL2368733 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL504699 Ki = 0.06 nM 10.22
CHEMBL497064 Ki = 0.09 nM 10.05
CHEMBL296512 Ki = 0.09 nM 10.05
CHEMBL497054 Ki = 0.11 nM 9.96
CHEMBL523245 Ki = 0.12 nM 9.92
CHEMBL496860 Ki = 0.23 nM 9.64
CHEMBL507898 Ki = 0.25 nM 9.60
CHEMBL496687 Ki = 0.34 nM 9.47
CHEMBL523760 Ki = 0.35 nM 9.46
CHEMBL497877 Ki = 0.43 nM 9.37
CHEMBL498729 Ki = 0.46 nM 9.34
CHEMBL40584 Ki = 0.48 nM 9.32
CHEMBL2368734 Ki = 0.54 nM 9.27
CHEMBL523585 Ki = 0.69 nM 9.16
CHEMBL42557 Ki = 0.99 nM 9.00
CHEMBL2113667 Ki = 1.2 nM 8.92
CHEMBL498048 Ki = 2.3 nM 8.64
CHEMBL2368748 Ki = 3.3 nM 8.48
CHEMBL497878 Ki = 4.0 nM 8.40
CHEMBL43819 Ki = 4.7 nM 8.33
CHEMBL496852 Ki = 10.2 nM 7.99
CHEMBL507727 Ki = 10.4 nM 7.98
CHEMBL295559 Ki = 12.0 nM 7.92
CHEMBL43697 Ki = 14.0 nM 7.85
CHEMBL40284 Ki = 18.0 nM 7.75
CHEMBL46523 Ki = 20.0 nM 7.70
CHEMBL295596 Ki = 26.0 nM 7.58
CHEMBL44310 Ki = 59.0 nM 7.23
CHEMBL2368745 Ki = 70.0 nM 7.16
CHEMBL2368733 Ki = 220.0 nM 6.66
CHEMBL40229 Ki = 320.0 nM 6.50