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Assay Detail

CHEMBL616556

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

Binding
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
20
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 1B (CHEMBL3459)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 20 5.05 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL11265 3 5.89
CHEMBL422283 1 5.66
CHEMBL133375 1 5.57
CHEMBL135952 1 5.42
CHEMBL137643 1 5.36
CHEMBL11592 3 5.30
CHEMBL422453 1 4.96
CHEMBL283606 1 4.70
CHEMBL8412 IPSAPIRONE 2.0 1 4.30
CHEMBL137486 1 4.29
CHEMBL137478 1 4.16
CHEMBL135490 1 -
CHEMBL132970 1 -
CHEMBL135489 1 -
CHEMBL135335 1 -
CHEMBL137642 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL11265 IC50 = 1300.0 nM 5.89
CHEMBL422283 IC50 = 2210.0 nM 5.66
CHEMBL133375 IC50 = 2700.0 nM 5.57
CHEMBL135952 IC50 = 3800.0 nM 5.42
CHEMBL11265 IC50 = 3800.0 nM 5.42
CHEMBL137643 IC50 = 4400.0 nM 5.36
CHEMBL11592 IC50 = 5000.0 nM 5.30
CHEMBL11592 IC50 = 6000.0 nM 5.22
CHEMBL11592 IC50 = 10000.0 nM 5.00
CHEMBL422453 IC50 = 11000.0 nM 4.96
CHEMBL283606 IC50 = 20000.0 nM 4.70
CHEMBL11265 IC50 = 31100.0 nM 4.51
CHEMBL8412 IPSAPIRONE IC50 = 50000.0 nM 4.30
CHEMBL137486 IC50 = 51100.0 nM 4.29
CHEMBL137478 IC50 = 69100.0 nM 4.16
CHEMBL137642 IC50 > 1000000.0 nM -
CHEMBL135335 IC50 = 246000.0 nM -
CHEMBL135489 IC50 > 100000.0 nM -
CHEMBL132970 IC50 > 100000.0 nM -
CHEMBL135490 IC50 > 1000000.0 nM -