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Assay Detail

CHEMBL4000282

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

Binding
Displacement of [3H]ketanserin from human 5-HT2A receptor expressed in F1pIn CHO cell membranes after 1 hr by scintillation counting method
12
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Proof of concept study for designed multiple ligands targeting the dopamine D2, serotonin 5-HT2A, and muscarinic M1 acetylcholine receptors.
Szabo M, Lim HD, Herenbrink CK, Christopoulos A, Lane JR, Capuano B.
J Med Chem (2015) 58 : 1550 -1555
PubMed 25590655 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.12 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4062602 2 8.57
CHEMBL4090568 2 8.24
CHEMBL4093980 2 7.12
CHEMBL4066435 2 6.56
CHEMBL4104013 2 6.25
CHEMBL1242923 2 5.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4062602 Ki = 2.692 nM 8.57
CHEMBL4062602 Ki = 2.7 nM 8.57
CHEMBL4090568 Ki = 5.754 nM 8.24
CHEMBL4090568 Ki = 5.8 nM 8.24
CHEMBL4093980 Ki = 75.86 nM 7.12
CHEMBL4093980 Ki = 75.8 nM 7.12
CHEMBL4066435 Ki = 275.42 nM 6.56
CHEMBL4066435 Ki = 275.0 nM 6.56
CHEMBL4104013 Ki = 562.34 nM 6.25
CHEMBL4104013 Ki = 568.0 nM 6.25
CHEMBL1242923 Ki = 1047.13 nM 5.98
CHEMBL1242923 Ki = 1042.0 nM 5.98