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Assay Detail

CHEMBL3705078

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Binding
Radioligand Binding Assay: The TAAR1 radioligand 3[H]-(S)-4-[(ethyl-phenyl-amino)-methyl]-4,5-dihydro-oxazol-2-ylamine (described in WO 2008/098857) was used at a concentration equal to the calculated Kd value, that was usually around 0.7 nM, resulting in the binding of approximately 0.5% of the radioligand and a specific binding representing approximately 70% of the total binding. Nonspecific binding was defined as the amount of 3[H]-(S)-4-[(ethyl-phenyl-amino)-methyl]-4,5-dihydro-oxazol-2-ylamine bound in the presence of 10 μM unlabeled ligand.
ChEMBL ↗
75
Total Activities
75
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Trace amine-associated receptor 1 (CHEMBL4908) ↗
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Dihydrooxazol-2-amine derivatives
(2014)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 75 8.29 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3656483 — — 1 10.00
CHEMBL3656531 — — 1 9.70
CHEMBL3656479 — — 1 9.70
CHEMBL3656481 — — 1 9.70
CHEMBL3656492 — — 1 9.70
CHEMBL3656484 — — 1 9.70
CHEMBL3656527 — — 1 9.52
CHEMBL3656496 — — 1 9.52
CHEMBL3656533 — — 1 9.52
CHEMBL3656488 — — 1 9.30
CHEMBL3656530 — — 1 9.30
CHEMBL3656524 — — 1 9.22
CHEMBL3656534 — — 1 9.15
CHEMBL3656499 — — 1 9.15
CHEMBL3656522 — — 1 9.15
CHEMBL3656487 — — 1 9.10
CHEMBL3656515 — — 1 9.10
CHEMBL3656501 — — 1 9.00
CHEMBL3656517 — — 1 9.00
CHEMBL3656491 — — 1 8.92
CHEMBL3656486 — — 1 8.89
CHEMBL3656510 — — 1 8.89
CHEMBL3656490 — — 1 8.89
CHEMBL3656489 — — 1 8.82
CHEMBL3656480 — — 1 8.77
CHEMBL3660707 — — 1 8.72
CHEMBL3656505 — — 1 8.72
CHEMBL3656529 — — 1 8.72
CHEMBL3656475 — — 1 8.68
CHEMBL3656477 — — 1 8.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3656483 — Ki = 0.1 nM 10.00
CHEMBL3656531 — Ki = 0.2 nM 9.70
CHEMBL3656479 — Ki = 0.2 nM 9.70
CHEMBL3656481 — Ki = 0.2 nM 9.70
CHEMBL3656492 — Ki = 0.2 nM 9.70
CHEMBL3656484 — Ki = 0.2 nM 9.70
CHEMBL3656527 — Ki = 0.3 nM 9.52
CHEMBL3656496 — Ki = 0.3 nM 9.52
CHEMBL3656533 — Ki = 0.3 nM 9.52
CHEMBL3656488 — Ki = 0.5 nM 9.30
CHEMBL3656530 — Ki = 0.5 nM 9.30
CHEMBL3656524 — Ki = 0.6 nM 9.22
CHEMBL3656499 — Ki = 0.7 nM 9.15
CHEMBL3656522 — Ki = 0.7 nM 9.15
CHEMBL3656534 — Ki = 0.7 nM 9.15
CHEMBL3656487 — Ki = 0.8 nM 9.10
CHEMBL3656515 — Ki = 0.8 nM 9.10
CHEMBL3656501 — Ki = 1.0 nM 9.00
CHEMBL3656517 — Ki = 1.0 nM 9.00
CHEMBL3656491 — Ki = 1.2 nM 8.92
CHEMBL3656486 — Ki = 1.3 nM 8.89
CHEMBL3656510 — Ki = 1.3 nM 8.89
CHEMBL3656490 — Ki = 1.3 nM 8.89
CHEMBL3656489 — Ki = 1.5 nM 8.82
CHEMBL3656480 — Ki = 1.7 nM 8.77
CHEMBL3660707 — Ki = 1.9 nM 8.72
CHEMBL3656529 — Ki = 1.9 nM 8.72
CHEMBL3656505 — Ki = 1.9 nM 8.72
CHEMBL3656475 — Ki = 2.1 nM 8.68
CHEMBL3656477 — Ki = 2.1 nM 8.68
CHEMBL3656476 — Ki = 2.2 nM 8.66
CHEMBL3656513 — Ki = 2.4 nM 8.62
CHEMBL3656482 — Ki = 3.2 nM 8.49
CHEMBL3656495 — Ki = 3.4 nM 8.47
CHEMBL3656498 — Ki = 3.5 nM 8.46
CHEMBL3656474 — Ki = 3.5 nM 8.46
CHEMBL3656525 — Ki = 4.6 nM 8.34
CHEMBL3656509 — Ki = 4.7 nM 8.33
CHEMBL3656528 — Ki = 5.0 nM 8.30
CHEMBL3656511 — Ki = 7.0 nM 8.15
CHEMBL3656518 — Ki = 7.7 nM 8.11
CHEMBL3656532 — Ki = 8.0 nM 8.10
CHEMBL3660699 — Ki = 8.4 nM 8.08
CHEMBL3656506 — Ki = 9.6 nM 8.02
CHEMBL3656519 — Ki = 10.5 nM 7.98
CHEMBL3656512 — Ki = 12.8 nM 7.89
CHEMBL3656504 — Ki = 13.3 nM 7.88
CHEMBL3660706 — Ki = 13.7 nM 7.86
CHEMBL3656521 — Ki = 16.6 nM 7.78
CHEMBL3656497 — Ki = 18.2 nM 7.74