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Assay Detail

CHEMBL617143

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

Binding
Binding affinity to 5-hydroxytryptamine 2 receptor using calf frontal cortex, [3H]- ketanserin, and spiperone for NSB
23
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

3-amino-3,4-dihydro-2H-1-benzopyran derivatives as 5-HT1A receptor ligands and potential anxiolytic agents. 2. Synthesis and quantitative structure-activity relationship studies of spiro[pyrrolidine- and piperidine-2,3'(2'H)-benzopyrans]
Comoy C, Marot C, Podona T, Baudin ML, Morin-Allory L, Guillaumet G, Pfeiffer B, Caignard DH, Renard P, Rettori MC, Adam G, Guardiola-Lemaitre B.
J Med Chem (1996) 39 : 4285 -4298
PubMed 8863806 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 4.99 6.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL11265 3 6.05
CHEMBL11592 3 6.00
CHEMBL422283 1 5.54
CHEMBL135952 1 5.22
CHEMBL8412 IPSAPIRONE 2.0 1 5.12
CHEMBL334498 1 5.08
CHEMBL49 BUSPIRONE 4.0 1 5.00
CHEMBL137486 1 4.68
CHEMBL137478 1 4.38
CHEMBL56 8-OH-DPAT 1 4.31
CHEMBL283606 1 4.22
CHEMBL133375 1 4.17
CHEMBL137643 1 4.15
CHEMBL137642 1 -
CHEMBL422453 1 -
CHEMBL135335 1 -
CHEMBL135489 1 -
CHEMBL132970 1 -
CHEMBL135490 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL11265 IC50 = 886.0 nM 6.05
CHEMBL11592 IC50 = 1000.0 nM 6.00
CHEMBL422283 IC50 = 2910.0 nM 5.54
CHEMBL11592 IC50 = 3000.0 nM 5.52
CHEMBL11592 IC50 = 5000.0 nM 5.30
CHEMBL135952 IC50 = 5950.0 nM 5.22
CHEMBL11265 IC50 = 6610.0 nM 5.18
CHEMBL8412 IPSAPIRONE IC50 = 7500.0 nM 5.12
CHEMBL334498 IC50 = 8390.0 nM 5.08
CHEMBL49 BUSPIRONE IC50 = 10000.0 nM 5.00
CHEMBL11265 IC50 = 13900.0 nM 4.86
CHEMBL137486 IC50 = 21100.0 nM 4.68
CHEMBL137478 IC50 = 41400.0 nM 4.38
CHEMBL56 8-OH-DPAT IC50 = 49000.0 nM 4.31
CHEMBL283606 IC50 = 60000.0 nM 4.22
CHEMBL133375 IC50 = 67300.0 nM 4.17
CHEMBL137643 IC50 = 71400.0 nM 4.15
CHEMBL135489 IC50 = 364000.0 nM -
CHEMBL135335 IC50 > 1000000.0 nM -
CHEMBL132970 IC50 > 1000000.0 nM -
CHEMBL422453 IC50 = 112000.0 nM -
CHEMBL135490 IC50 = 233000.0 nM -
CHEMBL137642 IC50 = 793000.0 nM -