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Assay Detail

CHEMBL2213071

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

Binding
Displacement of (S)-4-(2,4-difluorophenyl-3-tritio) -4,5-dihydro-2-oxazolamine from human TAAR1 receptor expressed in HEK293 cells after 90 mins by beta counting analysis
ChEMBL ↗
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Optimisation of imidazole compounds as selective TAAR1 agonists: discovery of RO5073012.
Galley G, Stalder H, Goergler A, Hoener MC, Norcross RD.
Bioorg Med Chem Lett (2012) 22 : 5244 -5248
PubMed 22795332 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 47 7.14 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2206385 — — 1 8.70
CHEMBL2206400 — — 1 8.70
CHEMBL2206890 — — 1 8.40
CHEMBL2206376 — — 1 8.40
CHEMBL2206377 — — 1 8.40
CHEMBL2206381 — — 1 8.30
CHEMBL2206375 — — 1 8.22
CHEMBL2206402 — — 1 7.96
CHEMBL2206384 — — 1 7.96
CHEMBL2206408 — — 1 7.92
CHEMBL2206379 — — 1 7.92
CHEMBL2206388 — — 1 7.92
CHEMBL2206380 — — 1 7.89
CHEMBL2206378 — — 1 7.75
CHEMBL494421 — — 1 7.70
CHEMBL2206404 — — 1 7.66
CHEMBL2206397 — — 1 7.62
CHEMBL348369 — — 1 7.50
CHEMBL2206386 — — 1 7.48
CHEMBL2206407 — — 1 7.46
CHEMBL2206396 — — 1 7.44
CHEMBL2206889 — — 1 7.40
CHEMBL2206403 — — 1 7.32
CHEMBL2206401 — — 1 7.19
CHEMBL2206371 — — 1 7.17
CHEMBL2206405 — — 1 7.16
CHEMBL2206382 — — 1 7.10
CHEMBL71033 — — 1 7.09
CHEMBL2206390 — — 1 7.08
CHEMBL2206406 — — 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2206385 — Ki = 2.0 nM 8.70
CHEMBL2206400 — Ki = 2.0 nM 8.70
CHEMBL2206376 — Ki = 4.0 nM 8.40
CHEMBL2206377 — Ki = 4.0 nM 8.40
CHEMBL2206890 — Ki = 4.0 nM 8.40
CHEMBL2206381 — Ki = 5.0 nM 8.30
CHEMBL2206375 — Ki = 6.0 nM 8.22
CHEMBL2206402 — Ki = 11.0 nM 7.96
CHEMBL2206384 — Ki = 11.0 nM 7.96
CHEMBL2206408 — Ki = 12.0 nM 7.92
CHEMBL2206379 — Ki = 12.0 nM 7.92
CHEMBL2206388 — Ki = 12.0 nM 7.92
CHEMBL2206380 — Ki = 13.0 nM 7.89
CHEMBL2206378 — Ki = 18.0 nM 7.75
CHEMBL494421 — Ki = 20.0 nM 7.70
CHEMBL2206404 — Ki = 22.0 nM 7.66
CHEMBL2206397 — Ki = 24.0 nM 7.62
CHEMBL348369 — Ki = 32.0 nM 7.50
CHEMBL2206386 — Ki = 33.0 nM 7.48
CHEMBL2206407 — Ki = 35.0 nM 7.46
CHEMBL2206396 — Ki = 36.0 nM 7.44
CHEMBL2206889 — Ki = 40.0 nM 7.40
CHEMBL2206403 — Ki = 48.0 nM 7.32
CHEMBL2206401 — Ki = 65.0 nM 7.19
CHEMBL2206371 — Ki = 68.0 nM 7.17
CHEMBL2206405 — Ki = 69.0 nM 7.16
CHEMBL2206382 — Ki = 80.0 nM 7.10
CHEMBL71033 — Ki = 82.0 nM 7.09
CHEMBL2206390 — Ki = 84.0 nM 7.08
CHEMBL2206406 — Ki = 100.0 nM 7.00
CHEMBL2206389 — Ki = 100.0 nM 7.00
CHEMBL2206383 — Ki = 128.0 nM 6.89
CHEMBL2206369 — Ki = 138.0 nM 6.86
CHEMBL2206387 — Ki = 195.0 nM 6.71
CHEMBL2206391 — Ki = 300.0 nM 6.52
CHEMBL2206394 — Ki = 400.0 nM 6.40
CHEMBL2206370 — Ki = 470.0 nM 6.33
CHEMBL149652 — Ki = 500.0 nM 6.30
CHEMBL2206398 — Ki = 630.0 nM 6.20
CHEMBL2206372 — Ki = 710.0 nM 6.15
CHEMBL2206392 — Ki = 825.0 nM 6.08
CHEMBL2206373 — Ki = 1270.0 nM 5.90
CHEMBL2206395 — Ki = 1390.0 nM 5.86
CHEMBL770 TOLAZOLINE Ki = 1640.0 nM 5.79
CHEMBL2206374 — Ki = 4250.0 nM 5.37
CHEMBL2206399 — Ki = 13300.0 nM 4.88
CHEMBL2206393 — Ki = 43000.0 nM 4.37