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Assay Detail

CHEMBL1259255

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

Functional
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
74
Total Activities
73
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists.
Bollinger S, Hübner H, Heinemann FW, Meyer K, Gmeiner P.
J Med Chem (2010) 53 : 7167 -7179
PubMed 20860381 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 74 7.38 8.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1259155 1 8.18
CHEMBL1259124 1 8.07
CHEMBL1259241 1 8.00
CHEMBL1259209 1 7.96
CHEMBL1259033 1 7.92
CHEMBL1259151 1 7.89
CHEMBL1259034 1 7.82
CHEMBL1258999 1 7.80
CHEMBL1259071 1 7.77
CHEMBL1259200 1 7.75
CHEMBL1259032 1 7.75
CHEMBL1259087 1 7.70
CHEMBL1259107 1 7.70
CHEMBL1259210 1 7.58
CHEMBL1259072 1 7.52
CHEMBL1259139 1 7.52
CHEMBL1259184 1 7.50
CHEMBL1259016 1 7.47
CHEMBL1259122 1 7.46
CHEMBL1259036 1 7.44
CHEMBL1259109 1 7.41
CHEMBL1259121 1 7.38
CHEMBL1259138 1 7.34
CHEMBL1259223 1 7.33
CHEMBL1259224 1 7.32
CHEMBL1259198 1 7.30
CHEMBL1259181 1 7.28
CHEMBL1259153 1 7.27
CHEMBL1259123 1 7.23
CHEMBL1255610 1 7.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1259155 EC50 = 6.6 nM 8.18
CHEMBL1259124 EC50 = 8.6 nM 8.07
CHEMBL1259241 EC50 = 10.0 nM 8.00
CHEMBL1259209 EC50 = 11.0 nM 7.96
CHEMBL1259033 EC50 = 12.0 nM 7.92
CHEMBL1259151 EC50 = 13.0 nM 7.89
CHEMBL1259034 EC50 = 15.0 nM 7.82
CHEMBL1258999 EC50 = 16.0 nM 7.80
CHEMBL1259071 EC50 = 17.0 nM 7.77
CHEMBL1259200 EC50 = 18.0 nM 7.75
CHEMBL1259032 EC50 = 18.0 nM 7.75
CHEMBL1259107 EC50 = 20.0 nM 7.70
CHEMBL1259087 EC50 = 20.0 nM 7.70
CHEMBL1259210 EC50 = 26.0 nM 7.58
CHEMBL1259139 EC50 = 30.0 nM 7.52
CHEMBL1259072 EC50 = 30.0 nM 7.52
CHEMBL1259184 EC50 = 32.0 nM 7.50
CHEMBL1259016 EC50 = 34.0 nM 7.47
CHEMBL1259122 EC50 = 35.0 nM 7.46
CHEMBL1259036 EC50 = 36.0 nM 7.44
CHEMBL1259109 EC50 = 39.0 nM 7.41
CHEMBL1259121 EC50 = 42.0 nM 7.38
CHEMBL1259138 EC50 = 46.0 nM 7.34
CHEMBL1259223 EC50 = 47.0 nM 7.33
CHEMBL1259224 EC50 = 48.0 nM 7.32
CHEMBL1259198 EC50 = 50.0 nM 7.30
CHEMBL1259181 EC50 = 52.0 nM 7.28
CHEMBL1259153 EC50 = 54.0 nM 7.27
CHEMBL1259123 EC50 = 59.0 nM 7.23
CHEMBL1255610 EC50 = 62.0 nM 7.21
CHEMBL1259090 EC50 = 63.0 nM 7.20
CHEMBL1259089 EC50 = 86.0 nM 7.07
CHEMBL1259035 EC50 = 93.0 nM 7.03
CHEMBL1259165 EC50 = 99.0 nM 7.00
CHEMBL1259055 EC50 = 100.0 nM 7.00
CHEMBL1259108 EC50 = 130.0 nM 6.89
CHEMBL1259051 EC50 = 240.0 nM 6.62
CHEMBL1259242 EC50 = 240.0 nM 6.62
CHEMBL3084757 EC50 = 270.0 nM 6.57
CHEMBL1259017 EC50 = 310.0 nM 6.51
CHEMBL1258996 EC50 = 600.0 nM 6.22
CHEMBL1259073 EC50 - -
CHEMBL1259182 EC50 - -
CHEMBL3084758 EC50 - -
CHEMBL3084758 EC50 - -
CHEMBL1259168 EC50 - -
CHEMBL1259054 EC50 - -
CHEMBL1259074 EC50 - -
CHEMBL1259167 EC50 - -
CHEMBL1259150 EC50 - -