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Assay Detail

CHEMBL621531

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

Binding
Binding affinity against rat 5-hydroxytryptamine 2A receptor using [3H]ketanserin as radioligand
29
Total Activities
29
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 2A (CHEMBL322)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

1-[2-methoxy-5-(3-phenylpropyl)]-2-aminopropane unexpectedly shows 5-HT(2A) serotonin receptor affinity and antagonist character.
Rangisetty JB, Dukat M, Dowd CS, Herrick-Davis K, DuPre A, Gadepalli S, Teitler M, Kelley CR, Sharif NA, Glennon RA.
J Med Chem (2001) 44 : 3283 -3291
PubMed 11563927 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 6.75 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL105381 1 8.10
CHEMBL113215 1 7.89
CHEMBL110151 1 7.75
CHEMBL326565 1 7.70
CHEMBL111061 1 7.64
CHEMBL8334 1 7.52
CHEMBL6607 BROLAMFETAMINE 2.0 1 7.50
CHEMBL111708 1 7.34
CHEMBL110740 1 7.23
CHEMBL109589 1 7.14
CHEMBL112590 1 7.05
CHEMBL109763 1 7.04
CHEMBL112768 1 6.96
CHEMBL327128 1 6.76
CHEMBL419563 1 6.75
CHEMBL322357 1 6.62
CHEMBL332919 1 6.53
CHEMBL110802 1 6.53
CHEMBL112792 1 6.46
CHEMBL111912 1 6.42
CHEMBL114445 1 6.36
CHEMBL320725 1 6.22
CHEMBL112653 1 6.16
CHEMBL54254 1 6.00
CHEMBL287047 1 5.55
CHEMBL321471 1 5.46
CHEMBL111361 1 5.22
CHEMBL322262 1 5.17
CHEMBL100635 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL105381 Ki = 8.0 nM 8.10
CHEMBL113215 Ki = 13.0 nM 7.89
CHEMBL110151 Ki = 18.0 nM 7.75
CHEMBL326565 Ki = 20.0 nM 7.70
CHEMBL111061 Ki = 23.0 nM 7.64
CHEMBL8334 Ki = 30.0 nM 7.52
CHEMBL6607 BROLAMFETAMINE Ki = 32.0 nM 7.50
CHEMBL111708 Ki = 46.0 nM 7.34
CHEMBL110740 Ki = 59.0 nM 7.23
CHEMBL109589 Ki = 72.0 nM 7.14
CHEMBL112590 Ki = 89.0 nM 7.05
CHEMBL109763 Ki = 91.0 nM 7.04
CHEMBL112768 Ki = 110.0 nM 6.96
CHEMBL327128 Ki = 172.0 nM 6.76
CHEMBL419563 Ki = 176.0 nM 6.75
CHEMBL322357 Ki = 240.0 nM 6.62
CHEMBL332919 Ki = 295.0 nM 6.53
CHEMBL110802 Ki = 295.0 nM 6.53
CHEMBL112792 Ki = 345.0 nM 6.46
CHEMBL111912 Ki = 380.0 nM 6.42
CHEMBL114445 Ki = 438.0 nM 6.36
CHEMBL320725 Ki = 600.0 nM 6.22
CHEMBL112653 Ki = 700.0 nM 6.16
CHEMBL54254 Ki = 1000.0 nM 6.00
CHEMBL287047 Ki = 2820.0 nM 5.55
CHEMBL321471 Ki = 3460.0 nM 5.46
CHEMBL111361 Ki = 5960.0 nM 5.22
CHEMBL322262 Ki = 6720.0 nM 5.17
CHEMBL100635 Ki > 10000.0 nM -