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Assay Detail

CHEMBL617674

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

Binding
Tested for binding affinity against 5-hydroxytryptamine 2 receptor from rat frontal cortical regions using [3H]ketanserin as radioligand
25
Total Activities
25
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

Antagonism of 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane stimulus with a newly identified 5-HT2- versus 5-HT1C-selective antagonist.
Ismaiel AM, De Los Angeles J, Teitler M, Ingher S, Glennon RA.
J Med Chem (1993) 36 : 2519 -2525
PubMed 8355253 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 7.26 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267930 SPIPERONE 2.0 1 9.00
CHEMBL79834 SPIRAMIDE 2.0 1 8.70
CHEMBL316004 LENPERONE 2.0 1 8.40
CHEMBL314702 1 8.30
CHEMBL84542 1 8.30
CHEMBL86072 1 8.10
CHEMBL419848 1 7.52
CHEMBL315522 1 7.50
CHEMBL314430 1 7.47
CHEMBL82688 1 7.30
CHEMBL85954 1 7.16
CHEMBL85508 1 7.16
CHEMBL83867 1 7.10
CHEMBL85507 1 7.06
CHEMBL313337 1 7.02
CHEMBL82519 PRIMAPERONE 2.0 1 6.85
CHEMBL309484 1 6.64
CHEMBL85392 1 6.53
CHEMBL82436 1 6.49
CHEMBL84079 1 6.24
CHEMBL309992 1 6.22
CHEMBL81959 1 6.00
CHEMBL82565 1 5.85
CHEMBL82567 1 -
CHEMBL309711 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267930 SPIPERONE Ki = 1.0 nM 9.00
CHEMBL79834 SPIRAMIDE Ki = 2.0 nM 8.70
CHEMBL316004 LENPERONE Ki = 4.0 nM 8.40
CHEMBL314702 Ki = 5.0 nM 8.30
CHEMBL84542 Ki = 5.0 nM 8.30
CHEMBL86072 Ki = 8.0 nM 8.10
CHEMBL419848 Ki = 30.0 nM 7.52
CHEMBL315522 Ki = 32.0 nM 7.50
CHEMBL314430 Ki = 34.0 nM 7.47
CHEMBL82688 Ki = 50.0 nM 7.30
CHEMBL85954 Ki = 70.0 nM 7.16
CHEMBL85508 Ki = 70.0 nM 7.16
CHEMBL83867 Ki = 80.0 nM 7.10
CHEMBL85507 Ki = 88.0 nM 7.06
CHEMBL313337 Ki = 95.0 nM 7.02
CHEMBL82519 PRIMAPERONE Ki = 140.0 nM 6.85
CHEMBL309484 Ki = 230.0 nM 6.64
CHEMBL85392 Ki = 295.0 nM 6.53
CHEMBL82436 Ki = 325.0 nM 6.49
CHEMBL84079 Ki = 570.0 nM 6.24
CHEMBL309992 Ki = 600.0 nM 6.22
CHEMBL81959 Ki = 1000.0 nM 6.00
CHEMBL82565 Ki = 1400.0 nM 5.85
CHEMBL82567 Ki > 100000.0 nM -
CHEMBL309711 Ki > 10000.0 nM -