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Assay Detail

CHEMBL3293223

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

Binding
Displacement of [3Hprazosin from adrenergic alpha1 receptor in pig cerebral cortex homogenates by competitive binding assay
ChEMBL ↗
53
Total Activities
21
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Tissue Cerebral cortex
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

Functionally selective dopamine D₂, D₃ receptor partial agonists.
Möller D, Kling RC, Skultety M, Leuner K, Hübner H, Gmeiner P.
J Med Chem (2014) 57 : 4861 -4875
PubMed 24831693 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 32 7.04 8.89
Ki 21 7.63 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3287403 — — 6 8.89
CHEMBL2028019 CARIPRAZINE 4.0 3 8.51
CHEMBL3287396 — — 3 8.29
CHEMBL3287404 — — 3 8.10
CHEMBL3287399 — — 3 8.01
CHEMBL3287392 — — 3 8.00
CHEMBL3287401 — — 1 7.96
CHEMBL3287405 — — 3 7.89
CHEMBL3287393 — — 1 7.82
CHEMBL3287400 — — 1 7.82
CHEMBL3287406 — — 3 7.80
CHEMBL1112 ARIPIPRAZOLE 4.0 3 7.77
CHEMBL3287397 — — 3 7.75
CHEMBL3287402 — — 3 7.75
CHEMBL3287398 — — 1 7.70
CHEMBL3287391 — — 1 7.66
CHEMBL3287394 — — 1 7.64
CHEMBL3287395 — — 3 7.37
CHEMBL3287390 — — 3 7.21
CHEMBL59 DOPAMINE 4.0 2 6.51
CHEMBL240773 QUINPIROLE 2.0 3 6.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3287403 — EC50 = 1.3 nM 8.89
CHEMBL3287403 — EC50 = 1.349 nM 8.87
CHEMBL3287403 — Ki = 2.9 nM 8.54
CHEMBL2028019 CARIPRAZINE EC50 = 3.1 nM 8.51
CHEMBL2028019 CARIPRAZINE EC50 = 3.09 nM 8.51
CHEMBL3287396 — Ki = 5.1 nM 8.29
CHEMBL3287403 — Ki = 6.6 nM 8.18
CHEMBL3287403 — EC50 = 7.2 nM 8.14
CHEMBL3287403 — EC50 = 7.244 nM 8.14
CHEMBL3287404 — Ki = 8.0 nM 8.10
CHEMBL3287399 — Ki = 9.7 nM 8.01
CHEMBL3287392 — EC50 = 10.0 nM 8.00
CHEMBL3287392 — EC50 = 10.0 nM 8.00
CHEMBL3287401 — Ki = 11.0 nM 7.96
CHEMBL3287405 — Ki = 13.0 nM 7.89
CHEMBL3287400 — Ki = 15.0 nM 7.82
CHEMBL3287393 — Ki = 15.0 nM 7.82
CHEMBL3287406 — Ki = 16.0 nM 7.80
CHEMBL1112 ARIPIPRAZOLE Ki = 17.0 nM 7.77
CHEMBL3287397 — Ki = 18.0 nM 7.75
CHEMBL3287402 — Ki = 18.0 nM 7.75
CHEMBL3287398 — Ki = 20.0 nM 7.70
CHEMBL3287399 — EC50 = 20.0 nM 7.70
CHEMBL3287399 — EC50 = 19.95 nM 7.70
CHEMBL3287391 — Ki = 22.0 nM 7.66
CHEMBL3287394 — Ki = 23.0 nM 7.64
CHEMBL3287392 — Ki = 28.0 nM 7.55
CHEMBL1112 ARIPIPRAZOLE EC50 = 39.0 nM 7.41
CHEMBL1112 ARIPIPRAZOLE EC50 = 38.9 nM 7.41
CHEMBL3287395 — Ki = 43.0 nM 7.37
CHEMBL3287390 — Ki = 62.0 nM 7.21
CHEMBL3287405 — EC50 = 63.1 nM 7.20
CHEMBL3287405 — EC50 = 64.0 nM 7.19
CHEMBL2028019 CARIPRAZINE Ki = 70.0 nM 7.16
CHEMBL3287397 — EC50 = 186.21 nM 6.73
CHEMBL3287397 — EC50 = 190.0 nM 6.72
CHEMBL3287396 — EC50 = 257.04 nM 6.59
CHEMBL3287396 — EC50 = 260.0 nM 6.58
CHEMBL59 DOPAMINE EC50 = 310.0 nM 6.51
CHEMBL59 DOPAMINE EC50 = 309.03 nM 6.51
CHEMBL3287390 — EC50 = 354.81 nM 6.45
CHEMBL3287390 — EC50 = 360.0 nM 6.44
CHEMBL3287402 — EC50 = 616.6 nM 6.21
CHEMBL3287404 — EC50 = 616.6 nM 6.21
CHEMBL3287402 — EC50 = 620.0 nM 6.21
CHEMBL240773 QUINPIROLE EC50 = 610.0 nM 6.21
CHEMBL3287404 — EC50 = 610.0 nM 6.21
CHEMBL240773 QUINPIROLE EC50 = 616.6 nM 6.21
CHEMBL3287395 — EC50 = 741.31 nM 6.13
CHEMBL3287395 — EC50 = 740.0 nM 6.13