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Assay Detail

CHEMBL4671578

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Binding
Binding affinity to human dopamine D1 receptor
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(1A) dopamine receptor (CHEMBL2056)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and pharmacological evaluation of 11-(1,6-dimethyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepines with clozapine-like receptor occupancy at dopamine D/D receptor.
Watanabe H,Ishida K,Yamamoto M,Horiguchi M,Isobe Y
Bioorg Med Chem Lett (2020) 30 : 127563 -127563
PubMed 32976928 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 8.33 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3039528 ZICRONAPINE 3.0 1 9.89
CHEMBL4758723 1 9.70
CHEMBL4756254 1 9.32
CHEMBL298406 ECOPIPAM 3.0 1 9.05
CHEMBL4795230 1 9.05
CHEMBL4742056 1 8.96
CHEMBL4760903 1 8.85
CHEMBL4740880 1 8.80
CHEMBL4745489 1 8.70
CHEMBL4757297 1 8.70
CHEMBL4745124 1 8.64
CHEMBL4797375 1 8.62
CHEMBL4758966 1 8.43
CHEMBL4756987 1 8.40
CHEMBL4776090 1 8.26
CHEMBL4793813 1 8.10
CHEMBL42 CLOZAPINE 4.0 1 7.36
CHEMBL715 OLANZAPINE 4.0 1 7.33
CHEMBL4779001 1 7.29
CHEMBL4782694 1 7.26
CHEMBL4748915 1 6.42
CHEMBL4753299 1 6.11
CHEMBL4745242 1 -
CHEMBL4779083 1 -
CHEMBL4784005 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3039528 ZICRONAPINE Ki = 0.13 nM 9.89
CHEMBL4758723 Ki = 0.2 nM 9.70
CHEMBL4756254 Ki = 0.48 nM 9.32
CHEMBL298406 ECOPIPAM Ki = 0.9 nM 9.05
CHEMBL4795230 Ki = 0.9 nM 9.05
CHEMBL4742056 Ki = 1.1 nM 8.96
CHEMBL4760903 Ki = 1.4 nM 8.85
CHEMBL4740880 Ki = 1.6 nM 8.80
CHEMBL4745489 Ki = 2.0 nM 8.70
CHEMBL4757297 Ki = 2.0 nM 8.70
CHEMBL4745124 Ki = 2.3 nM 8.64
CHEMBL4797375 Ki = 2.4 nM 8.62
CHEMBL4758966 Ki = 3.7 nM 8.43
CHEMBL4756987 Ki = 4.0 nM 8.40
CHEMBL4776090 Ki = 5.5 nM 8.26
CHEMBL4793813 Ki = 7.9 nM 8.10
CHEMBL42 CLOZAPINE Ki = 44.0 nM 7.36
CHEMBL715 OLANZAPINE Ki = 47.0 nM 7.33
CHEMBL4779001 Ki = 51.0 nM 7.29
CHEMBL4782694 Ki = 55.0 nM 7.26
CHEMBL4748915 Ki = 380.0 nM 6.42
CHEMBL4753299 Ki = 780.0 nM 6.11
CHEMBL4745242 Ki - -
CHEMBL4779083 Ki - -
CHEMBL4784005 Ki - -