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Assay Detail

CHEMBL617142

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

Binding
Binding affinity towards 5-hydroxytryptamine 2 receptor in calf frontal cortex
44
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Frontal cortex
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

5-hydroxytryptamine receptor 2A (CHEMBL3446)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

3,4-Dihydro-3-amino-2H-1-benzopyran derivatives as 5-HT1A receptor ligands and potential anxiolytic agents. 1. Synthesis and structure--activity relationship studies.
Podona T, Guardiola-Lemaître B, Caignard DH, Adam G, Pfeiffer B, Renard P, Guillaumet G.
J Med Chem (1994) 37 : 1779 -1793
PubMed 7912735 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 44 5.23 6.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL296395 1 6.22
CHEMBL50188 1 6.10
CHEMBL51888 3 6.00
CHEMBL52785 1 6.00
CHEMBL301060 3 6.00
CHEMBL299561 1 5.70
CHEMBL50993 1 5.70
CHEMBL417550 1 5.52
CHEMBL50530 3 5.52
CHEMBL298534 1 5.52
CHEMBL27763 1 5.40
CHEMBL50722 1 5.40
CHEMBL48925 1 5.40
CHEMBL283606 3 5.40
CHEMBL300735 3 5.30
CHEMBL52485 1 5.22
CHEMBL553833 1 5.22
CHEMBL54266 1 5.22
CHEMBL8412 IPSAPIRONE 2.0 1 5.12
CHEMBL54089 1 5.10
CHEMBL52438 1 5.00
CHEMBL49 BUSPIRONE 4.0 1 5.00
CHEMBL284912 1 5.00
CHEMBL51561 1 5.00
CHEMBL52396 1 4.52
CHEMBL56 8-OH-DPAT 1 4.31
CHEMBL285010 1 4.22
CHEMBL25984 1 4.10
CHEMBL545198 1 -
CHEMBL50841 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL296395 IC50 = 600.0 nM 6.22
CHEMBL50188 IC50 = 800.0 nM 6.10
CHEMBL51888 IC50 = 1000.0 nM 6.00
CHEMBL52785 IC50 = 1000.0 nM 6.00
CHEMBL301060 IC50 = 1000.0 nM 6.00
CHEMBL299561 IC50 = 2000.0 nM 5.70
CHEMBL50993 IC50 = 2000.0 nM 5.70
CHEMBL50530 IC50 = 3000.0 nM 5.52
CHEMBL417550 IC50 = 3000.0 nM 5.52
CHEMBL301060 IC50 = 3000.0 nM 5.52
CHEMBL298534 IC50 = 3000.0 nM 5.52
CHEMBL48925 IC50 = 4000.0 nM 5.40
CHEMBL50722 IC50 = 4000.0 nM 5.40
CHEMBL27763 IC50 = 4000.0 nM 5.40
CHEMBL283606 IC50 = 4000.0 nM 5.40
CHEMBL300735 IC50 = 5000.0 nM 5.30
CHEMBL301060 IC50 = 5000.0 nM 5.30
CHEMBL52485 IC50 = 6000.0 nM 5.22
CHEMBL553833 IC50 = 6000.0 nM 5.22
CHEMBL54266 IC50 = 6000.0 nM 5.22
CHEMBL8412 IPSAPIRONE IC50 = 7500.0 nM 5.12
CHEMBL54089 IC50 = 8000.0 nM 5.10
CHEMBL300735 IC50 = 8000.0 nM 5.10
CHEMBL50530 IC50 = 9000.0 nM 5.05
CHEMBL283606 IC50 = 9700.0 nM 5.01
CHEMBL51561 IC50 = 10000.0 nM 5.00
CHEMBL52438 IC50 = 10000.0 nM 5.00
CHEMBL49 BUSPIRONE IC50 = 10000.0 nM 5.00
CHEMBL50530 IC50 = 10000.0 nM 5.00
CHEMBL284912 IC50 = 10000.0 nM 5.00
CHEMBL300735 IC50 = 10000.0 nM 5.00
CHEMBL51888 IC50 = 10000.0 nM 5.00
CHEMBL52396 IC50 = 30000.0 nM 4.52
CHEMBL56 8-OH-DPAT IC50 = 49000.0 nM 4.31
CHEMBL285010 IC50 = 60000.0 nM 4.22
CHEMBL283606 IC50 = 60000.0 nM 4.22
CHEMBL25984 IC50 = 80000.0 nM 4.10
CHEMBL545198 IC50 > 100000.0 nM -
CHEMBL264027 IC50 > 1000000.0 nM -
CHEMBL27995 IC50 > 100000.0 nM -
CHEMBL51888 IC50 > 1000000.0 nM -
CHEMBL50841 IC50 > 1000000.0 nM -
CHEMBL51985 IC50 > 1000000.0 nM -
CHEMBL416747 IC50 > 1000000.0 nM -