Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL617242

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

Binding
Affinity for 5-hydroxytryptamine 2 receptor binding sites by its ability to displace [3H]spiperone from rat frontal cortex.
51
Total Activities
51
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

3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).
Strupczewski JT, Bordeau KJ, Chiang Y, Glamkowski EJ, Conway PG, Corbett R, Hartman HB, Szewczak MR, Wilmot CA, Helsley GC.
J Med Chem (1995) 38 : 1119 -1131
PubMed 7707315 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 51 7.70 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL276799 1 9.15
CHEMBL273307 1 9.05
CHEMBL14610 1 8.70
CHEMBL85 RISPERIDONE 4.0 1 8.59
CHEMBL14380 1 8.54
CHEMBL14148 1 8.49
CHEMBL279996 1 8.46
CHEMBL436141 1 8.42
CHEMBL14470 1 8.42
CHEMBL273907 1 8.31
CHEMBL14539 1 8.28
CHEMBL14415 1 8.28
CHEMBL14322 1 8.26
CHEMBL274039 1 8.07
CHEMBL14376 ILOPERIDONE 4.0 1 8.05
CHEMBL14163 1 7.96
CHEMBL14510 1 7.80
CHEMBL14077 1 7.80
CHEMBL14100 1 7.77
CHEMBL14727 1 7.75
CHEMBL14393 1 7.70
CHEMBL14681 1 7.70
CHEMBL275016 1 7.70
CHEMBL14394 1 7.66
CHEMBL14365 1 7.64
CHEMBL274462 1 7.58
CHEMBL427822 1 7.48
CHEMBL274223 1 7.47
CHEMBL417620 1 7.44
CHEMBL14389 1 7.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL276799 IC50 = 0.7 nM 9.15
CHEMBL273307 IC50 = 0.9 nM 9.05
CHEMBL14610 IC50 = 2.0 nM 8.70
CHEMBL85 RISPERIDONE IC50 = 2.6 nM 8.59
CHEMBL14380 IC50 = 2.9 nM 8.54
CHEMBL14148 IC50 = 3.2 nM 8.49
CHEMBL279996 IC50 = 3.5 nM 8.46
CHEMBL436141 IC50 = 3.8 nM 8.42
CHEMBL14470 IC50 = 3.8 nM 8.42
CHEMBL273907 IC50 = 4.9 nM 8.31
CHEMBL14539 IC50 = 5.2 nM 8.28
CHEMBL14415 IC50 = 5.2 nM 8.28
CHEMBL14322 IC50 = 5.5 nM 8.26
CHEMBL274039 IC50 = 8.5 nM 8.07
CHEMBL14376 ILOPERIDONE IC50 = 9.0 nM 8.05
CHEMBL14163 IC50 = 11.0 nM 7.96
CHEMBL14510 IC50 = 16.0 nM 7.80
CHEMBL14077 IC50 = 16.0 nM 7.80
CHEMBL14100 IC50 = 17.0 nM 7.77
CHEMBL14727 IC50 = 18.0 nM 7.75
CHEMBL14393 IC50 = 20.0 nM 7.70
CHEMBL14681 IC50 = 20.0 nM 7.70
CHEMBL275016 IC50 = 20.0 nM 7.70
CHEMBL14394 IC50 = 22.0 nM 7.66
CHEMBL14365 IC50 = 23.0 nM 7.64
CHEMBL274462 IC50 = 26.0 nM 7.58
CHEMBL427822 IC50 = 33.0 nM 7.48
CHEMBL274223 IC50 = 34.0 nM 7.47
CHEMBL417620 IC50 = 36.0 nM 7.44
CHEMBL14389 IC50 = 38.0 nM 7.42
CHEMBL14538 IC50 = 40.0 nM 7.40
CHEMBL273633 IC50 = 41.0 nM 7.39
CHEMBL14306 IC50 = 42.0 nM 7.38
CHEMBL14509 IC50 = 45.0 nM 7.35
CHEMBL14361 IC50 = 45.0 nM 7.35
CHEMBL14246 IC50 = 49.0 nM 7.31
CHEMBL42 CLOZAPINE IC50 = 50.0 nM 7.30
CHEMBL14219 IC50 = 53.0 nM 7.28
CHEMBL14158 IC50 = 63.0 nM 7.20
CHEMBL276750 IC50 = 67.0 nM 7.17
CHEMBL14556 IC50 = 67.0 nM 7.17
CHEMBL14348 IC50 = 89.0 nM 7.05
CHEMBL14043 IC50 = 91.0 nM 7.04
CHEMBL14522 IC50 = 122.0 nM 6.91
CHEMBL14206 IC50 = 143.0 nM 6.84
CHEMBL14494 IC50 = 153.0 nM 6.82
CHEMBL54 HALOPERIDOL IC50 = 170.0 nM 6.77
CHEMBL275064 IC50 = 170.0 nM 6.77
CHEMBL14218 IC50 = 241.0 nM 6.62
CHEMBL14395 IC50 < 10.0 nM -