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Assay Detail

CHEMBL989986

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Functional
Agonist activity at human trace amine associated receptor 1 expressed in RD-HGA16 CHO-K1 cells coexpressed with Galpha16 protein assessed as internal calcium mobilization by calcium 3 assay
69
Total Activities
69
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Trace amine-associated receptor 1 (CHEMBL5857)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity correlations for beta-phenethylamines at human trace amine receptor 1.
Lewin AH, Navarro HA, Mascarella SW.
Bioorg Med Chem (2008) 16 : 7415 -7423
PubMed 18602830 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 68 5.90 7.29
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL510649 1 7.29
CHEMBL447753 1 7.24
CHEMBL379916 1 7.19
CHEMBL407939 1 7.11
CHEMBL476517 1 6.99
CHEMBL443141 1 6.93
CHEMBL610 PHENETHYLAMINE 1 6.89
CHEMBL448232 1 6.89
CHEMBL100635 1 6.84
CHEMBL446238 1 6.82
CHEMBL453667 1 6.80
CHEMBL274497 1 6.72
CHEMBL478847 1 6.69
CHEMBL452901 1 6.51
CHEMBL451372 1 6.45
CHEMBL508991 1 6.44
CHEMBL509695 1 6.42
CHEMBL45763 1 6.41
CHEMBL505644 1 6.40
CHEMBL130703 1 6.30
CHEMBL446131 1 6.28
CHEMBL367501 1 6.21
CHEMBL448576 1 6.20
CHEMBL478845 1 6.16
CHEMBL11608 TYRAMINE 3.0 1 6.14
CHEMBL217315 1 6.13
CHEMBL450477 1 6.12
CHEMBL19393 LEVAMFETAMINE 4.0 1 6.04
CHEMBL612 DEXTROAMPHETAMINE 4.0 1 6.03
CHEMBL476324 1 5.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL510649 EC50 = 51.0 nM 7.29
CHEMBL447753 EC50 = 57.0 nM 7.24
CHEMBL379916 EC50 = 65.0 nM 7.19
CHEMBL407939 EC50 = 77.0 nM 7.11
CHEMBL476517 EC50 = 103.0 nM 6.99
CHEMBL443141 EC50 = 117.0 nM 6.93
CHEMBL610 PHENETHYLAMINE EC50 = 129.0 nM 6.89
CHEMBL448232 EC50 = 129.0 nM 6.89
CHEMBL100635 EC50 = 144.0 nM 6.84
CHEMBL446238 EC50 = 150.0 nM 6.82
CHEMBL453667 EC50 = 160.0 nM 6.80
CHEMBL274497 EC50 = 189.0 nM 6.72
CHEMBL478847 EC50 = 205.0 nM 6.69
CHEMBL452901 EC50 = 312.0 nM 6.51
CHEMBL451372 EC50 = 355.0 nM 6.45
CHEMBL508991 EC50 = 361.0 nM 6.44
CHEMBL509695 EC50 = 377.0 nM 6.42
CHEMBL45763 EC50 = 387.0 nM 6.41
CHEMBL505644 EC50 = 398.0 nM 6.40
CHEMBL130703 EC50 = 501.0 nM 6.30
CHEMBL446131 EC50 = 530.0 nM 6.28
CHEMBL367501 EC50 = 614.0 nM 6.21
CHEMBL448576 EC50 = 638.0 nM 6.20
CHEMBL478845 EC50 = 687.0 nM 6.16
CHEMBL11608 TYRAMINE EC50 = 731.0 nM 6.14
CHEMBL217315 EC50 = 740.0 nM 6.13
CHEMBL450477 EC50 = 767.0 nM 6.12
CHEMBL19393 LEVAMFETAMINE EC50 = 920.0 nM 6.04
CHEMBL612 DEXTROAMPHETAMINE EC50 = 935.0 nM 6.03
CHEMBL476324 EC50 = 1040.0 nM 5.98
CHEMBL476750 EC50 = 1070.0 nM 5.97
CHEMBL442603 EC50 = 1160.0 nM 5.94
CHEMBL449727 EC50 = 1290.0 nM 5.89
CHEMBL509223 EC50 = 1400.0 nM 5.85
CHEMBL316698 EC50 = 1444.0 nM 5.84
CHEMBL1179 EC50 = 1510.0 nM 5.82
CHEMBL476516 EC50 = 1540.0 nM 5.81
CHEMBL145584 EC50 = 1740.0 nM 5.76
CHEMBL287047 EC50 = 2010.0 nM 5.70
CHEMBL477764 EC50 = 2860.0 nM 5.54
CHEMBL10780 EC50 = 3400.0 nM 5.47
CHEMBL147230 EC50 = 3430.0 nM 5.46
CHEMBL506244 EC50 = 3460.0 nM 5.46
CHEMBL124733 EC50 = 3750.0 nM 5.43
CHEMBL448523 EC50 = 3950.0 nM 5.40
CHEMBL450561 EC50 = 4320.0 nM 5.37
CHEMBL103299 EC50 = 4380.0 nM 5.36
CHEMBL420095 EC50 = 5030.0 nM 5.30
CHEMBL61251 EC50 = 5050.0 nM 5.30
CHEMBL1574 PHENTERMINE EC50 = 5470.0 nM 5.26