|
|
CCCCC1=NC2(CCCC2)C(=O)N1CC3=CC=C(C=C3)C4=CC=CC=C4C#N |
Approved |
|
Arntl (gene)
,
PER3
|
Angiotensin receptor binding,
PER3
|
|
|
|
C1=CC=C2C(=C1)C=CC3=CC4=CC=CC=C4C=C32 |
None |
|
CRY1-PER2 complex
,
CLOCK-BMAL1
,
Arntl (gene)
|
Disruption of circadian clock,
Interferes with CLOCK–BMAL1,
aryl hydrocarbon receptor (AhR) binding
|
|
|
|
C1=CC=C2C(=C1)C=C3C=CC4=C5C3=C2C6=CC=CC=C6C5=CC=C4 |
none |
|
mPer2
,
mPer1
,
CRY1-PER2 complex
,
CRY1
,
CLOCK-BMAL1
,
Arntl (gene)
|
Disruption of circadian clock,
Core clock suppression,
Interferes with CLOCK–BMAL1,
Targets BMAL1–CLOCK DNA-binding activity,
aryl hydrocarbon receptor (AhR) binding
|
|
|
|
C1=CC=C2C=C3C=CC=CC3=CC2=C1 |
none |
|
CRY1-PER2 complex
,
CLOCK-BMAL1
|
Disruption of circadian clock,
Core clock suppression,
Interferes with CLOCK–BMAL1,
aryl hydrocarbon receptor (AhR) binding
|
|
|
|
C1=CC=C2C=CC=CC2=C1 |
none |
|
CLOCK-BMAL1
|
Core clock modulation,
Core clock suppression,
Bmal1,
BMAL1 expression modulation
|
|
|
|
CC1=C(C2=CC3=C(C(=C([N-]3)C=C4C(=C(C(=N4)C=C5C(=C(C(=N5)C=C1[N-]2)C)C=C)C)C=C)C)CCC(=O)O)CCC(=O)O.[Fe+2] |
Not approved |
|
CLOCK-BMAL1
|
Serves as a cofactor in various hemoproteins (e.g., hemoglobin, cytochromes) and can modulate transcription factors (e.g., REV-E
|
|
|
|
COC1=CC(=CC(=C1)/C=C/C2=CC=C(C=C2)O)OC |
Not approved |
|
mPer2
,
mPer1
,
CRY1-PER2 complex
,
CRY1
,
CLOCK-BMAL1
,
Arntl (gene)
,
BMAL1 expression (induction)
|
Core clock modulation,
Bmal1,
de-repressing BMAL1,
BMAL1 expression modulation,
BMAL1 expression modulation,
Activation of CLOCK/Bmal1 mediated transcription,
SIRT1-mediated peroxisome proliferator-activated receptor coactivator 1α (PGC-1α) deacetylation in sleep-restricted mice
|
|
|
|
CCCCCNC(=O)N1CCC(C1)CN(CC2=CC=C(C=C2)Cl)CC3=CC=C(S3)[N+](=O)[O-] |
none |
|
mPer2
,
REV-ERBα
,
BMAL1 expression (induction)
,
Per2 expression
|
Agonist REV-ERB alpha
|
|
|
|
CC(C)(C)OC(=O)CN(CC1=CC=C(C=C1)Cl)CC2=CC=C(S2)[N+](=O)[O-] |
none |
|
REV-ERBα
|
Antagonist of Rev-Erb nuclear receptors
|
|
|
|
CC(C1=CC(=C(C=C1)OC)OC)C(=O)C2=C(C=C(C=C2)C(C)(C)C#C)OC |
none |
|
CLOCK-BMAL1
|
Core clock modulation,
Bmal1,
BMAL1 expression modulation
|
|
|
|
C[C@@H]1[C@H]([C@H](C[C@@H](O1)O[C@@H]2[C@H](O[C@H](C[C@@H]2O)O[C@@H]3[C@H](O[C@H](C[C@@H]3O)O[C@H]4CC[C@]5([C@@H](C4)CC[C@@H]6[C@@H]5C[C@H]([C@]7([C@@]6(CC[C@@H]7C8=CC(=O)OC8)O)C)O)C)C)C)O)O |
Approved |
|
ROR gamma
|
ROR,
RORγ binding
|
|
|
|
CC1=CC=C(C=C1)N2C(=O)N(C(=O)S2)CC3=CC=C(C=C3)F |
none |
|
ROR gamma
|
ROR,
RORγ binding
|
|
|
|
C[C@H]1[C@H]2[C@H](C[C@@H]3[C@@]2(CC[C@H]4[C@H]3CC=C5[C@@]4([C@@H](C[C@@H](C5)O)O)C)C)O[C@]16CCC(=C)CO6 |
none |
|
RORA
,
RORα
,
NR1F1
|
ROR
|
|
|
|
COC1=C(C=C(C=C1)C2=CC(=O)C3=C(O2)C(=C(C(=C3OC)OC)OC)OC)OC |
Not approved |
|
RORA
|
Core clock modulation,
ROR,
PER gene exspression modulation,
Activation of CLOCK/Bmal1 mediated transcription
|
|
|
|
C1=CC=C(C=C1)C(C2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NCC3=CC=C(C=C3)O |
Not approved |
|
Neuropeptide Y Y1 receptor
|
Neuropeptide Y1 receptor binding
|
|
|
|
CCC1=CC=C(C=C1)N(CC(C)C)S(=O)(=O)C2=CC(=C(C=C2)OCC3CCOCC3)CO |
none |
|
ROR gamma
|
ROR,
RORγ binding
|
|
|
|
CC(C)NCCN(C(C)C)S(=O)(=O)C1=C(C=C(C=C1)Cl)Cl |
Not approved |
|
TRPV4 Channel
|
This inhibition of TRPV4-mediated signaling can affect downstream pathways involved in the regulation of the circadian clock.
|
|
|
|
CC(=O)N1CC2=C([C@@H]1C(=O)NC3=CC=C(C=C3)C(C(F)(F)F)(C(F)(F)F)O)C=CC(=C2)S(=O)(=O)C |
None |
|
ROR gamma
|
ROR,
RORγ binding
|
|
|
|
COC1=C(C=C2CC(C(=O)C2=C1)CC3=C(C=CC=N3)C(F)(F)F)N4CCOCC4 |
None |
|
ROR gamma
|
ROR
|
|
|
|
CCS(=O)(=O)C1=CN=C(C=C1)CNC(=O)C2=CC3=C([C@H](N(C3)CC4CCC(CC4)C(F)(F)F)C(C)C)N=C2 |
Not approved |
|
ROR gamma
|
RORyt/RORc inhibitor
|
|
|
|
CC(C)N1C=NC2=C1N=CN=C2N(CC3=CC(=CC=C3)C(F)(F)F)CC4=C(C=CC=C4)[N+](=O)[O-] |
None |
|
CKI delta
|
Inhibits CKIδ
|
|
|
|
C1COCCC1N2C3=NC=NC(=C3C(=N2)COC4=CC(=CC=C4)Cl)N |
Not approved |
|
CK1δ
|
CK1 Inhibition
|
|
|
|
CC1=CC2=C(C=C1Cl)N=C(S2)NC(=O)CC3=CC=CC=C 3 |
None |
|
CKI delta
|
Inhibits casein kinase 1 delta (CKIδ) activity,
Inhibits CKIδ
|
|
|
|
C1=CC(=CC(=C1)Cl)NC2=NC3=C(C=CC(=C3)C(=O)O)C4=C2C=CN=C4 |
Not approved |
|
CK1δ
|
Binds to the ATP‑binding site of CK2
|
|
|
|
COC1=CC(=C(CN(C2=C3N=CN(C3=NC=N2)C(C)C)CC2=CC(=CC=C2)C(F)(F)F)C=C1OC)[N+](=O)[O-] |
none |
|
CKI delta
|
Inhibits casein kinase 1 delta (CKIδ) activity,
Inhibits CKIδ
|
|