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Assay Detail

CHEMBL1176404

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

Binding
Selectivity ratio of Ki for human cloned 5HT2C receptor to Ki for human cloned 5HT2A receptor
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Serotonin 2 receptors; 5-HT2a & 5-HT2c (CHEMBL2096662)
Type SELECTIVITY GROUP
Organism Homo sapiens

Publication

Synthesis and structure-affinity relationships of novel small molecule natural product derivatives capable of discriminating between serotonin 5-HT1A, 5-HT2A, 5-HT2C receptor subtypes.
Cummings DF, Canseco DC, Sheth P, Johnson JE, Schetz JA.
Bioorg Med Chem (2010) 18 : 4783 -4792
PubMed 20570529 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 34 7.79 10.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1172812 1 10.48
CHEMBL404232 APLYSINOPSIN 1 10.39
CHEMBL1173408 1 10.10
CHEMBL1173820 1 9.96
CHEMBL41347 1 8.22
CHEMBL93850 1 7.89
CHEMBL43916 1 7.80
CHEMBL42463 1 7.80
CHEMBL38911 1 7.80
CHEMBL296090 1 7.70
CHEMBL289063 1 7.60
CHEMBL42024 1 7.60
CHEMBL96883 1 7.60
CHEMBL328844 1 7.60
CHEMBL297043 1 7.50
CHEMBL43929 1 7.50
CHEMBL290395 1 7.50
CHEMBL276673 1 7.40
CHEMBL44095 1 7.40
CHEMBL92656 1 7.20
CHEMBL299530 1 7.10
CHEMBL299726 1 7.10
CHEMBL42276 1 7.00
CHEMBL40726 1 7.00
CHEMBL301784 1 6.90
CHEMBL433060 1 6.30
CHEMBL54769 1 5.90
CHEMBL1173333 1 -
CHEMBL463249 1 -
CHEMBL1173334 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1172812 Ki = 0.033 nM 10.48
CHEMBL404232 APLYSINOPSIN Ki = 0.041 nM 10.39
CHEMBL1173408 Ki = 0.079 nM 10.10
CHEMBL1173820 Ki = 0.11 nM 9.96
CHEMBL41347 Ki = 6.0 nM 8.22
CHEMBL93850 Ki = 13.0 nM 7.89
CHEMBL43916 Ki = 16.0 nM 7.80
CHEMBL42463 Ki = 16.0 nM 7.80
CHEMBL38911 Ki = 16.0 nM 7.80
CHEMBL296090 Ki = 20.0 nM 7.70
CHEMBL289063 Ki = 25.0 nM 7.60
CHEMBL42024 Ki = 25.0 nM 7.60
CHEMBL96883 Ki = 25.0 nM 7.60
CHEMBL328844 Ki = 25.0 nM 7.60
CHEMBL290395 Ki = 32.0 nM 7.50
CHEMBL297043 Ki = 32.0 nM 7.50
CHEMBL43929 Ki = 32.0 nM 7.50
CHEMBL276673 Ki = 40.0 nM 7.40
CHEMBL44095 Ki = 40.0 nM 7.40
CHEMBL92656 Ki = 63.0 nM 7.20
CHEMBL299530 Ki = 79.0 nM 7.10
CHEMBL299726 Ki = 80.0 nM 7.10
CHEMBL42276 Ki = 100.0 nM 7.00
CHEMBL40726 Ki = 100.0 nM 7.00
CHEMBL301784 Ki = 126.0 nM 6.90
CHEMBL433060 Ki = 502.0 nM 6.30
CHEMBL54769 Ki = 1260.0 nM 5.90
CHEMBL1173333 Ki > 602.0 nM -
CHEMBL463249 Ki > 45.0 nM -
CHEMBL1173334 Ki > 2170.0 nM -
CHEMBL56232 Ki > 100.0 nM -
CHEMBL55958 Ki > 251.0 nM -
CHEMBL59097 Ki > 1585.0 nM -
CHEMBL42327 Ki > 8.0 nM -