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Assay Detail

CHEMBL617687

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

Binding
The compound was tested in vitro for binding affinity towards 5-hydroxytryptamine 2 receptor by displacing [125]I-LSD radioligand
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Serotonin 2 (5-HT2) receptor (CHEMBL2093870)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Effect of N-alkylation on the affinities of analogues of spiperone for dopamine D2 and serotonin 5-HT2 receptors.
Mach RH, Jackson JR, Luedtke RR, Ivins KJ, Molinoff PB, Ehrenkaufer RL.
J Med Chem (1992) 35 : 423 -430
PubMed 1531364 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 8.62 10.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135917 1 10.02
CHEMBL334349 1 9.89
CHEMBL136942 1 9.51
CHEMBL136852 1 9.39
CHEMBL267930 SPIPERONE 2.0 1 9.35
CHEMBL267932 MESPIPERONE 2.0 1 9.26
CHEMBL135860 1 9.17
CHEMBL337149 1 9.00
CHEMBL135316 1 8.96
CHEMBL344399 1 8.89
CHEMBL135722 1 8.72
CHEMBL134400 1 8.49
CHEMBL137309 1 8.36
CHEMBL137648 1 8.28
CHEMBL135832 1 8.02
CHEMBL335606 1 7.92
CHEMBL337181 1 7.85
CHEMBL135500 1 7.72
CHEMBL538404 1 7.68
CHEMBL134545 1 7.43
CHEMBL335714 1 7.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135917 Ki = 0.096 nM 10.02
CHEMBL334349 Ki = 0.13 nM 9.89
CHEMBL136942 Ki = 0.31 nM 9.51
CHEMBL136852 Ki = 0.41 nM 9.39
CHEMBL267930 SPIPERONE Ki = 0.45 nM 9.35
CHEMBL267932 MESPIPERONE Ki = 0.55 nM 9.26
CHEMBL135860 Ki = 0.68 nM 9.17
CHEMBL337149 Ki = 1.0 nM 9.00
CHEMBL135316 Ki = 1.1 nM 8.96
CHEMBL344399 Ki = 1.3 nM 8.89
CHEMBL135722 Ki = 1.9 nM 8.72
CHEMBL134400 Ki = 3.2 nM 8.49
CHEMBL137309 Ki = 4.4 nM 8.36
CHEMBL137648 Ki = 5.3 nM 8.28
CHEMBL135832 Ki = 9.6 nM 8.02
CHEMBL335606 Ki = 12.0 nM 7.92
CHEMBL337181 Ki = 14.0 nM 7.85
CHEMBL135500 Ki = 19.0 nM 7.72
CHEMBL538404 Ki = 21.0 nM 7.68
CHEMBL134545 Ki = 37.0 nM 7.43
CHEMBL335714 Ki = 89.0 nM 7.05