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Assay Detail

CHEMBL961024

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

Binding
Displacement of [3H]MDL from rat 5HT2A receptor expressed in GF62 cells by liquid scintillation analyser
22
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type GF62
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 2A (CHEMBL322)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and in vitro affinities of various MDL 100907 derivatives as potential 18F-radioligands for 5-HT2A receptor imaging with PET.
Herth MM, Kramer V, Piel M, Palner M, Riss PJ, Knudsen GM, Rösch F.
Bioorg Med Chem (2009) 17 : 2989 -3002
PubMed 19329329 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 8.23 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL489621 1 9.60
CHEMBL492069 1 9.51
CHEMBL74355 VOLINANSERIN 3.0 2 9.42
CHEMBL515472 1 9.14
CHEMBL62919 ALTANSERIN 2.0 1 9.14
CHEMBL490847 1 8.91
CHEMBL489624 1 8.87
CHEMBL490846 1 8.79
CHEMBL476839 1 8.74
CHEMBL489634 1 8.69
CHEMBL516088 1 8.49
CHEMBL490632 1 8.34
CHEMBL402143 1 8.04
CHEMBL476838 1 7.58
CHEMBL492068 1 7.26
CHEMBL490633 1 7.23
CHEMBL522982 1 7.05
CHEMBL490634 1 6.93
CHEMBL489408 1 6.82
CHEMBL490845 1 5.70
CHEMBL489618 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL489621 Ki = 0.25 nM 9.60
CHEMBL492069 Ki = 0.31 nM 9.51
CHEMBL74355 VOLINANSERIN Ki = 0.38 nM 9.42
CHEMBL62919 ALTANSERIN Ki = 0.72 nM 9.14
CHEMBL515472 Ki = 0.72 nM 9.14
CHEMBL490847 Ki = 1.24 nM 8.91
CHEMBL489624 Ki = 1.34 nM 8.87
CHEMBL490846 Ki = 1.63 nM 8.79
CHEMBL476839 Ki = 1.83 nM 8.74
CHEMBL489634 Ki = 2.06 nM 8.69
CHEMBL74355 VOLINANSERIN Ki = 2.1 nM 8.68
CHEMBL516088 Ki = 3.23 nM 8.49
CHEMBL490632 Ki = 4.56 nM 8.34
CHEMBL402143 Ki = 9.02 nM 8.04
CHEMBL476838 Ki = 26.0 nM 7.58
CHEMBL492068 Ki = 55.0 nM 7.26
CHEMBL490633 Ki = 59.0 nM 7.23
CHEMBL522982 Ki = 90.0 nM 7.05
CHEMBL490634 Ki = 118.0 nM 6.93
CHEMBL489408 Ki = 153.0 nM 6.82
CHEMBL490845 Ki = 1987.0 nM 5.70
CHEMBL489618 Ki > 1000.0 nM -